211513-37-0,MFCD06407886
Catalog No.:AA00BF09

211513-37-0 | Dalcetrapib

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
≥98%
in stock  
$70.00   $49.00
- +
50mg
95%
in stock  
$284.00   $199.00
- +
100mg
95%
in stock  
$493.00   $345.00
- +
250mg
95%
in stock  
$970.00   $679.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA00BF09
Chemical Name:
Dalcetrapib
CAS Number:
211513-37-0
Molecular Formula:
C23H35NO2S
Molecular Weight:
389.5945
MDL Number:
MFCD06407886
SMILES:
CCC(CC1(CCCCC1)C(=O)Nc1ccccc1SC(=O)C(C)C)CC
Properties
Computed Properties
 
Complexity:
481  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
27  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
1  
Isotope Atom Count:
0  
Rotatable Bond Count:
9  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  
XLogP3:
7.1  

Downstream Synthesis Route

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

[2]CurrentPatentAssignee:JAPANTOBACCOINC-US6426365,2002,B1

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

Literature

Title: Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes.

Journal: The Journal of pharmacology and experimental therapeutics 20150401

Title: Future of cholesteryl ester transfer protein inhibitors.

Journal: Annual review of medicine 20140101

Title: Solubility and stability of dalcetrapib in vehicles and biological media.

Journal: International journal of pharmaceutics 20121101

Title: Evidence of a drug-drug interaction linked to inhibition of ester hydrolysis by orlistat.

Journal: Journal of cardiovascular pharmacology 20121001

Title: Tangier disease: epidemiology, pathophysiology, and management.

Journal: American journal of cardiovascular drugs : drugs, devices, and other interventions 20121001

Title: Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk.

Journal: Journal of lipid research 20120901

Title: Dalcetrapib , a cholesteryl ester transfer protein modulator.

Journal: Expert opinion on investigational drugs 20120901

Title: Rationale for cholesteryl ester transfer protein inhibition.

Journal: Current opinion in lipidology 20120801

Title: HDL and CETP Inhibition: Will This DEFINE the Future?

Journal: Current treatment options in cardiovascular medicine 20120801

Title: Lipid and apoprotein composition of HDL in partial or complete CETP deficiency.

Journal: Current vascular pharmacology 20120701

Title: Determination of dalcetrapib by liquid chromatography-tandem mass spectrometry.

Journal: Journal of pharmaceutical and biomedical analysis 20120701

Title: Increasing high-density lipoprotein cholesterol by cholesteryl ester transfer protein-inhibition: a rocky road and lessons learned? The early demise of the dal-HEART programme.

Journal: European heart journal 20120701

Title: An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels.

Journal: Future cardiology 20120701

Title: Current status of CETP inhibitors in the treatment of hyperlipidemia: an update.

Journal: Current clinical pharmacology 20120501

Title: Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20120501

Title: Dalcetrapib--restoring belief in modulating CETP as a beneficial mechanism in cardiovascular disease.

Journal: Expert opinion on investigational drugs 20120401

Title: Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial.

Journal: European heart journal 20120401

Title: Cholesteryl ester transfer protein inhibition and endothelial function: enough with the surrogates.

Journal: European heart journal 20120401

Title: No clinically relevant drug-drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30).

Journal: International journal of clinical pharmacology and therapeutics 20120401

Title: Monitoring Cyp2b10 mRNA expression at cessation of 2-year carcinogenesis bioassay in mouse liver provides evidence for a carcinogenic mechanism devoid of human relevance: the dalcetrapib experience.

Journal: Toxicology and applied pharmacology 20120315

Title: Pharmacotherapy. Elevating HDL-cholesterol levels with dalcetrapib is safe.

Journal: Nature reviews. Cardiology 20120306

Title: On- and off-target pharmacology of torcetrapib: current understanding and implications for the structure activity relationships (SAR), discovery and development of cholesteryl ester-transfer protein (CETP) inhibitors.

Journal: Drugs 20120305

Title: Effect of dalcetrapib plus pravastatin on lipoprotein metabolism and high-density lipoprotein composition and function in dyslipidemic patients: results of a phase IIb dose-ranging study.

Journal: American heart journal 20120301

Title: CETP inhibition in perspective.

Journal: Atherosclerosis 20120201

Title: New horizons for cholesterol ester transfer protein inhibitors.

Journal: Current atherosclerosis reports 20120201

Title: Efficacy and safety of dalcetrapib in type 2 diabetes mellitus and/or metabolic syndrome patients, at high cardiovascular disease risk.

Journal: Diabetes, obesity & metabolism 20120101

Title: Lipid exchange mechanism of the cholesteryl ester transfer protein clarified by atomistic and coarse-grained simulations.

Journal: PLoS computational biology 20120101

Title: Regulation of reverse cholesterol transport - a comprehensive appraisal of available animal studies.

Journal: Nutrition & metabolism 20120101

Title: Cholesteryl ester transfer-protein modulator and inhibitors and their potential for the treatment of cardiovascular diseases.

Journal: Vascular health and risk management 20120101

Title: Mipomersen: evidence-based review of its potential in the treatment of homozygous and severe heterozygous familial hypercholesterolemia.

Journal: Core evidence 20120101

Title: Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib.

Journal: Drug design, development and therapy 20120101

Title: Lipids, blood pressure, kidney - what was new in 2011?

Journal: Archives of medical science : AMS 20111231

Title: [Secondary coronary heart disease prevention. Will CEPT inhibitors be the next breakthrough?].

Journal: MMW Fortschritte der Medizin 20111208

Title: Cholesteryl ester transfer protein inhibition in cardiovascular risk management: ongoing trials will end the confusion.

Journal: Cardiovascular therapeutics 20111201

Title: Familial hypercholesterolemia: present and future management.

Journal: Current cardiology reports 20111201

Title: Multidimensional profiling of plasma lipoproteins by size exclusion chromatography followed by reverse-phase protein arrays.

Journal: Journal of lipid research 20111201

Title: Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects.

Journal: Atherosclerosis 20111201

Title: Cholesteryl ester transfer protein inhibition to reduce cardiovascular risk: Where are we now?

Journal: Trends in pharmacological sciences 20111201

Title: Therapy and clinical trials.

Journal: Current opinion in lipidology 20111201

Title: Investigational CETP antagonists for hyperlipidemia and atherosclerosis prevention.

Journal: Expert opinion on investigational drugs 20111101

Title: Safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-PLAQUE): a randomised clinical trial.

Journal: Lancet (London, England) 20111029

Title: Dalcetrapib: turning the tide for CETP inhibition?

Journal: Lancet (London, England) 20111029

Title: Anacetrapib: hope for CETP inhibitors?

Journal: Cardiovascular therapeutics 20111001

Title: Coronary artery disease: Dalcetrapib safely raises HDL-cholesterol level in the phase IIb dal-PLAQUE trial.

Journal: Nature reviews. Cardiology 20110927

Title: Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism.

Journal: Current opinion in lipidology 20110801

Title: Rationale and design of dal-PLAQUE: a study assessing efficacy and safety of dalcetrapib on progression or regression of atherosclerosis using magnetic resonance imaging and 18F-fluorodeoxyglucose positron emission tomography/computed tomography.

Journal: American heart journal 20110801

Title: Utility of atherosclerosis imaging in the evaluation of high-density lipoprotein-raising therapies.

Journal: Current atherosclerosis reports 20110601

Title: Triglyceride-rich lipoproteins and high-density lipoprotein cholesterol in patients at high risk of cardiovascular disease: evidence and guidance for management.

Journal: European heart journal 20110601

Title: Effects of food intake on the pharmacokinetic properties of dalcetrapib: findings from three phase I, single-dose crossover studies in healthy volunteers.

Journal: Clinical therapeutics 20110601

Title: [Cholesteryl ester transfer protein inhibition in the management of atherosclerotic cardiovascular disease: second act 'A rebirth of hope'].

Journal: Revista medica de Chile 20110601

Title: Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20110501

Title: Learning lessons from Pfizer's $800 million failure.

Journal: Nature reviews. Drug discovery 20110301

Title: Rationale and design of dal-VESSEL: a study to assess the safety and efficacy of dalcetrapib on endothelial function using brachial artery flow-mediated vasodilatation.

Journal: Current medical research and opinion 20110101

Title: Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors.

Journal: The Annals of pharmacotherapy 20110101

Title: [Novel therapy for atherosclerosis and inflammatory vascular disease].

Journal: Nihon rinsho. Japanese journal of clinical medicine 20110101

Title: Safety, tolerability and pharmacokinetics of dalcetrapib following single and multiple ascending doses in healthy subjects: a randomized, double-blind, placebo-controlled, phase I study.

Journal: Clinical drug investigation 20110101

Title: Primary prevention of coronary heart disease: integration of new data, evolving views, revised goals, and role of rosuvastatin in management. A comprehensive survey.

Journal: Drug design, development and therapy 20110101

Title: Where are we heading with noninvasive clinical vascular physiology? Why and how should we assess endothelial function?

Journal: Cardiology research and practice 20110101

Title: Emerging therapeutic strategies to enhance HDL function.

Journal: Lipids in health and disease 20110101

Title: Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport.

Journal: Journal of lipid research 20101201

Title: Lack of clinically relevant drug-drug interactions when dalcetrapib is co-administered with ezetimibe.

Journal: British journal of clinical pharmacology 20101201

Title: Good news for 'good' cholesterol.

Journal: Nature 20101118

Title: Coadministration of dalcetrapib with pravastatin, rosuvastatin, or simvastatin: no clinically relevant drug-drug interactions.

Journal: Journal of clinical pharmacology 20101001

Title: No clinically relevant drug-drug interactions when dalcetrapib is co-administered with atorvastatin.

Journal: Expert opinion on investigational drugs 20101001

Title: Emerging drugs for hyperlipidemia.

Journal: Expert opinion on emerging drugs 20100901

Title: Biochemical characterization of cholesteryl ester transfer protein inhibitors.

Journal: Journal of lipid research 20100901

Title: Mechanisms underlying off-target effects of the cholesteryl ester transfer protein inhibitor torcetrapib involve L-type calcium channels.

Journal: Journal of hypertension 20100801

Title: Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing.

Journal: European journal of clinical pharmacology 20100801

Title: Is a blood pressure rise the only deleterious off-target effect of cholesterol ester transfer protein inhibitors?

Journal: Journal of hypertension 20100801

Title: Dissociating HDL cholesterol from cardiovascular risk.

Journal: Lancet (London, England) 20100731

Title: Dalcetrapib: a review of Phase II data.

Journal: Expert opinion on investigational drugs 20100601

Title: High-density lipoprotein-mediated anti-atherosclerotic and endothelial-protective effects: a potential novel therapeutic target in cardiovascular disease.

Journal: Current pharmaceutical design 20100501

Title: Dalcetrapib: JTT 705; JTT-705; R 1658; R1658; RG1658; RO 4607381; RO4607381.

Journal: Drugs in R&D 20100501

Title: MARCO, a macrophage scavenger receptor highly expressed in rodents, mediates dalcetrapib-induced uptake of lipids by rat and mouse macrophages.

Journal: Toxicology in vitro : an international journal published in association with BIBRA 20100401

Title: [HDL and CETP in atherogenesis].

Journal: Deutsche medizinische Wochenschrift (1946) 20100201

Title: Functional assessment of HDL: Moving beyond static measures for risk assessment.

Journal: Cardiovascular drugs and therapy 20100201

Title: Safety and tolerability of dalcetrapib (RO4607381/JTT-705): results from a 48-week trial.

Journal: European heart journal 20100201

Title: Mulling over the odds of CETP inhibition.

Journal: European heart journal 20100201

Title: Cholesteryl ester transfer protein: at the heart of the action of lipid-modulating therapy with statins, fibrates, niacin, and cholesteryl ester transfer protein inhibitors.

Journal: European heart journal 20100101

Title: Insights from recent meta-analysis: role of high-density lipoprotein cholesterol in reducing cardiovascular events and rates of atherosclerotic disease progression.

Journal: Journal of clinical lipidology 20100101

Title: Update on CETP inhibition.

Journal: Journal of clinical lipidology 20100101

Title: Low high-density lipoprotein cholesterol: current status and future strategies for management.

Journal: Vascular health and risk management 20100101

Title: High density lipoproteins-based therapies for cardiovascular disease.

Journal: Journal of cardiovascular disease research 20100101

Title: Dalcetrapib: no off-target toxicity on blood pressure or on genes related to the renin-angiotensin-aldosterone system in rats.

Journal: British journal of pharmacology 20091201

Title: Rationale and design of the dal-OUTCOMES trial: efficacy and safety of dalcetrapib in patients with recent acute coronary syndrome.

Journal: American heart journal 20091201

Title: The pharmacology and off-target effects of some cholesterol ester transfer protein inhibitors.

Journal: The American journal of cardiology 20091116

Title: Mechanism of inhibition defines CETP activity: a mathematical model for CETP in vitro.

Journal: Journal of lipid research 20091101

Title: Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents.

Journal: Expert opinion on therapeutic patents 20090901

Title: Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis.

Journal: Current opinion in investigational drugs (London, England : 2000) 20090901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20090901

Title: Free thiol group of MD-2 as the target for inhibition of the lipopolysaccharide-induced cell activation.

Journal: The Journal of biological chemistry 20090717

Title: The end of the road for CETP inhibitors after torcetrapib?

Journal: Current opinion in cardiology 20090701

Title: Safety and tolerability of dalcetrapib.

Journal: The American journal of cardiology 20090701

Title: In vitro and in vivo assessment of the effect of dalcetrapib on a panel of CYP substrates.

Journal: Current medical research and opinion 20090401

Title: A single-center, open-label, one-sequence study of dalcetrapib coadministered with ketoconazole, and an in vitro study of the S-methyl metabolite of dalcetrapib.

Journal: Clinical therapeutics 20090301

Title: Cholesterylestertransfer protein inhibition and endothelial function in type II hyperlipidemia.

Journal: Thrombosis research 20090101

Title: JTT-705: is there still future for a CETP inhibitor after torcetrapib?

Journal: Expert opinion on investigational drugs 20081001

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20080501

Title: Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended?

Journal: Expert opinion on investigational drugs 20080401

Title: Is raising HDL a futile strategy for atheroprotection?

Journal: Nature reviews. Drug discovery 20080201

Title: HDL metabolism and CETP inhibition.

Journal: Cardiology in review 20080101

Title: Gateways to clinical trials. July-August 2008.

Journal: Methods and findings in experimental and clinical pharmacology 20080101

Title: The role of CETP inhibition in dyslipidemia.

Journal: Current atherosclerosis reports 20070801

Title: The biology and chemistry of hyperlipidemia.

Journal: Bioorganic & medicinal chemistry 20070715

Title: Cholesteryl ester transfer protein promotes the formation of cholesterol-rich remnant like lipoprotein particles in human plasma.

Journal: Clinica chimica acta; international journal of clinical chemistry 20070101

Title: Inhibition of CETP as a novel therapeutic strategy for reducing the risk of atherosclerotic disease.

Journal: European heart journal 20070101

Title: Therapeutic elevation of HDL-cholesterol to prevent atherosclerosis and coronary heart disease.

Journal: Pharmacology & therapeutics 20060901

Title: Cholesteryl ester transfer protein inhibition, high-density lipoprotein metabolism and heart disease risk reduction.

Journal: Current opinion in lipidology 20060801

Title: Are human CETP mutations and CETP-inhibiting drugs a good or a bad deal?

Journal: Journal of molecular medicine (Berlin, Germany) 20060801

Title: Raising high-density lipoprotein with cholesteryl ester transfer protein inhibitors.

Journal: Current opinion in pharmacology 20060401

Title: Targeting cholesteryl ester transfer protein for the prevention and management of cardiovascular disease.

Journal: Journal of the American College of Cardiology 20060207

Title: Increasing high-density lipoprotein cholesterol through cholesteryl Ester transfer protein inhibition: a next step in the fight against cardiovascular disease?

Journal: Current drug targets. Cardiovascular & haematological disorders 20051201

Title: JTT-705 blocks cell proliferation and angiogenesis through p38 kinase/p27(kip1) and Ras/p21(waf1) pathways.

Journal: Atherosclerosis 20051001

Title: Consequences of cholesteryl ester transfer protein inhibition in patients with familial hypoalphalipoproteinemia.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20050901

Title: Pharmacologic augmentation of high-density lipoproteins: mechanisms of currently available and emerging therapies.

Journal: Current opinion in cardiology 20050701

Title: Effectiveness of inhibition of cholesteryl ester transfer protein by JTT-705 in combination with pravastatin in type II dyslipidemia.

Journal: The American journal of cardiology 20050501

Title: Role of CETP inhibitors in the treatment of dyslipidemia.

Journal: Current opinion in lipidology 20041201

Title: Inhibition of cholesteryl ester transfer protein activity by JTT-705 increases apolipoprotein E-containing high-density lipoprotein and favorably affects the function and enzyme composition of high-density lipoprotein in rabbits.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20041001

Title: S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20040517

Title: JTT-705. Japan Tobacco.

Journal: Current opinion in investigational drugs (London, England : 2000) 20040301

Title: Inhibition of cholesteryl ester transfer protein increases serum apolipoprotein (apo) A-I levels by increasing the synthesis of apo A-I in rabbits.

Journal: Atherosclerosis 20040201

Title: Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells.

Journal: American journal of physiology. Endocrinology and metabolism 20030601

Title: Effect of JTT-705 on cholesteryl ester transfer protein and plasma lipid levels in normolipidemic animals.

Journal: European journal of pharmacology 20030411

Title: Cholesteryl ester transfer protein: a novel target for raising HDL and inhibiting atherosclerosis.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20030201

Title: Cholesteryl ester transfer protein inhibitor (JTT-705) and the development of atherosclerosis in rabbits with severe hypercholesterolaemia.

Journal: Clinical science (London, England : 1979) 20021201

Title: The Yin and Yang of cholesteryl ester transfer protein and atherosclerosis.

Journal: Clinical science (London, England : 1979) 20021201

Title: Efficacy and safety of a novel cholesteryl ester transfer protein inhibitor, JTT-705, in humans: a randomized phase II dose-response study.

Journal: Circulation 20020507

Title: Effect of HDL, from Japanese white rabbit administered a new cholesteryl ester transfer protein inhibitor JTT-705, on cholesteryl ester accumulation induced by acetylated low density lipoprotein in J774 macrophage.

Journal: Atherosclerosis 20020501

Title: [CETP inhibitor].

Journal: Nihon rinsho. Japanese journal of clinical medicine 20010301

Title: Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.

Title: Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572.

Title: Huang Z, et al. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219.

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Tags:211513-37-0 Molecular Formula|211513-37-0 MDL|211513-37-0 SMILES|211513-37-0 Dalcetrapib
Catalog No.: AA00BF09
211513-37-0,MFCD06407886
211513-37-0 | Dalcetrapib
Pack Size: 1mg
Purity: ≥98%
in stock
$70.00 $49.00
Pack Size: 50mg
Purity: 95%
in stock
$284.00 $199.00
Pack Size: 100mg
Purity: 95%
in stock
$493.00 $345.00
Pack Size: 250mg
Purity: 95%
in stock
$970.00 $679.00
Quantity
- +
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Technical Information
Catalog Number: AA00BF09
Chemical Name: Dalcetrapib
CAS Number: 211513-37-0
Molecular Formula: C23H35NO2S
Molecular Weight: 389.5945
MDL Number: MFCD06407886
SMILES: CCC(CC1(CCCCC1)C(=O)Nc1ccccc1SC(=O)C(C)C)CC
Properties
Complexity: 481  
Covalently-Bonded Unit Count: 1  
Defined Atom Stereocenter Count: 0  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 27  
Hydrogen Bond Acceptor Count: 3  
Hydrogen Bond Donor Count: 1  
Isotope Atom Count: 0  
Rotatable Bond Count: 9  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
XLogP3: 7.1  
Downstream Synthesis Route
79-30-1    211513-21-2    211513-37-0 

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

[2]CurrentPatentAssignee:JAPANTOBACCOINC-US6426365,2002,B1

381209-09-2    211513-37-0 

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

3814-34-4    211513-37-0 

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

211515-46-7    211513-37-0 

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

211513-15-4    211513-37-0 

[1]Shinkai;Maeda;Yamasaki;Okamoto;Uchida[JournalofMedicinalChemistry,2000,vol.43,#19,p.3566-3572]

Literature fold

Title: Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes.

Journal: The Journal of pharmacology and experimental therapeutics20150401

Title: Future of cholesteryl ester transfer protein inhibitors.

Journal: Annual review of medicine20140101

Title: Solubility and stability of dalcetrapib in vehicles and biological media.

Journal: International journal of pharmaceutics20121101

Title: Evidence of a drug-drug interaction linked to inhibition of ester hydrolysis by orlistat.

Journal: Journal of cardiovascular pharmacology20121001

Title: Tangier disease: epidemiology, pathophysiology, and management.

Journal: American journal of cardiovascular drugs : drugs, devices, and other interventions20121001

Title: Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk.

Journal: Journal of lipid research20120901

Title: Dalcetrapib , a cholesteryl ester transfer protein modulator.

Journal: Expert opinion on investigational drugs20120901

Title: Rationale for cholesteryl ester transfer protein inhibition.

Journal: Current opinion in lipidology20120801

Title: HDL and CETP Inhibition: Will This DEFINE the Future?

Journal: Current treatment options in cardiovascular medicine20120801

Title: Lipid and apoprotein composition of HDL in partial or complete CETP deficiency.

Journal: Current vascular pharmacology20120701

Title: Determination of dalcetrapib by liquid chromatography-tandem mass spectrometry.

Journal: Journal of pharmaceutical and biomedical analysis20120701

Title: Increasing high-density lipoprotein cholesterol by cholesteryl ester transfer protein-inhibition: a rocky road and lessons learned? The early demise of the dal-HEART programme.

Journal: European heart journal20120701

Title: An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels.

Journal: Future cardiology20120701

Title: Current status of CETP inhibitors in the treatment of hyperlipidemia: an update.

Journal: Current clinical pharmacology20120501

Title: Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

Journal: Bioorganic & medicinal chemistry letters20120501

Title: Dalcetrapib--restoring belief in modulating CETP as a beneficial mechanism in cardiovascular disease.

Journal: Expert opinion on investigational drugs20120401

Title: Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial.

Journal: European heart journal20120401

Title: Cholesteryl ester transfer protein inhibition and endothelial function: enough with the surrogates.

Journal: European heart journal20120401

Title: No clinically relevant drug-drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30).

Journal: International journal of clinical pharmacology and therapeutics20120401

Title: Monitoring Cyp2b10 mRNA expression at cessation of 2-year carcinogenesis bioassay in mouse liver provides evidence for a carcinogenic mechanism devoid of human relevance: the dalcetrapib experience.

Journal: Toxicology and applied pharmacology20120315

Title: Pharmacotherapy. Elevating HDL-cholesterol levels with dalcetrapib is safe.

Journal: Nature reviews. Cardiology20120306

Title: On- and off-target pharmacology of torcetrapib: current understanding and implications for the structure activity relationships (SAR), discovery and development of cholesteryl ester-transfer protein (CETP) inhibitors.

Journal: Drugs20120305

Title: Effect of dalcetrapib plus pravastatin on lipoprotein metabolism and high-density lipoprotein composition and function in dyslipidemic patients: results of a phase IIb dose-ranging study.

Journal: American heart journal20120301

Title: CETP inhibition in perspective.

Journal: Atherosclerosis20120201

Title: New horizons for cholesterol ester transfer protein inhibitors.

Journal: Current atherosclerosis reports20120201

Title: Efficacy and safety of dalcetrapib in type 2 diabetes mellitus and/or metabolic syndrome patients, at high cardiovascular disease risk.

Journal: Diabetes, obesity & metabolism20120101

Title: Lipid exchange mechanism of the cholesteryl ester transfer protein clarified by atomistic and coarse-grained simulations.

Journal: PLoS computational biology20120101

Title: Regulation of reverse cholesterol transport - a comprehensive appraisal of available animal studies.

Journal: Nutrition & metabolism20120101

Title: Cholesteryl ester transfer-protein modulator and inhibitors and their potential for the treatment of cardiovascular diseases.

Journal: Vascular health and risk management20120101

Title: Mipomersen: evidence-based review of its potential in the treatment of homozygous and severe heterozygous familial hypercholesterolemia.

Journal: Core evidence20120101

Title: Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib.

Journal: Drug design, development and therapy20120101

Title: Lipids, blood pressure, kidney - what was new in 2011?

Journal: Archives of medical science : AMS20111231

Title: [Secondary coronary heart disease prevention. Will CEPT inhibitors be the next breakthrough?].

Journal: MMW Fortschritte der Medizin20111208

Title: Cholesteryl ester transfer protein inhibition in cardiovascular risk management: ongoing trials will end the confusion.

Journal: Cardiovascular therapeutics20111201

Title: Familial hypercholesterolemia: present and future management.

Journal: Current cardiology reports20111201

Title: Multidimensional profiling of plasma lipoproteins by size exclusion chromatography followed by reverse-phase protein arrays.

Journal: Journal of lipid research20111201

Title: Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects.

Journal: Atherosclerosis20111201

Title: Cholesteryl ester transfer protein inhibition to reduce cardiovascular risk: Where are we now?

Journal: Trends in pharmacological sciences20111201

Title: Therapy and clinical trials.

Journal: Current opinion in lipidology20111201

Title: Investigational CETP antagonists for hyperlipidemia and atherosclerosis prevention.

Journal: Expert opinion on investigational drugs20111101

Title: Safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-PLAQUE): a randomised clinical trial.

Journal: Lancet (London, England)20111029

Title: Dalcetrapib: turning the tide for CETP inhibition?

Journal: Lancet (London, England)20111029

Title: Anacetrapib: hope for CETP inhibitors?

Journal: Cardiovascular therapeutics20111001

Title: Coronary artery disease: Dalcetrapib safely raises HDL-cholesterol level in the phase IIb dal-PLAQUE trial.

Journal: Nature reviews. Cardiology20110927

Title: Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism.

Journal: Current opinion in lipidology20110801

Title: Rationale and design of dal-PLAQUE: a study assessing efficacy and safety of dalcetrapib on progression or regression of atherosclerosis using magnetic resonance imaging and 18F-fluorodeoxyglucose positron emission tomography/computed tomography.

Journal: American heart journal20110801

Title: Utility of atherosclerosis imaging in the evaluation of high-density lipoprotein-raising therapies.

Journal: Current atherosclerosis reports20110601

Title: Triglyceride-rich lipoproteins and high-density lipoprotein cholesterol in patients at high risk of cardiovascular disease: evidence and guidance for management.

Journal: European heart journal20110601

Title: Effects of food intake on the pharmacokinetic properties of dalcetrapib: findings from three phase I, single-dose crossover studies in healthy volunteers.

Journal: Clinical therapeutics20110601

Title: [Cholesteryl ester transfer protein inhibition in the management of atherosclerotic cardiovascular disease: second act 'A rebirth of hope'].

Journal: Revista medica de Chile20110601

Title: Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey.

Journal: Xenobiotica; the fate of foreign compounds in biological systems20110501

Title: Learning lessons from Pfizer's $800 million failure.

Journal: Nature reviews. Drug discovery20110301

Title: Rationale and design of dal-VESSEL: a study to assess the safety and efficacy of dalcetrapib on endothelial function using brachial artery flow-mediated vasodilatation.

Journal: Current medical research and opinion20110101

Title: Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors.

Journal: The Annals of pharmacotherapy20110101

Title: [Novel therapy for atherosclerosis and inflammatory vascular disease].

Journal: Nihon rinsho. Japanese journal of clinical medicine20110101

Title: Safety, tolerability and pharmacokinetics of dalcetrapib following single and multiple ascending doses in healthy subjects: a randomized, double-blind, placebo-controlled, phase I study.

Journal: Clinical drug investigation20110101

Title: Primary prevention of coronary heart disease: integration of new data, evolving views, revised goals, and role of rosuvastatin in management. A comprehensive survey.

Journal: Drug design, development and therapy20110101

Title: Where are we heading with noninvasive clinical vascular physiology? Why and how should we assess endothelial function?

Journal: Cardiology research and practice20110101

Title: Emerging therapeutic strategies to enhance HDL function.

Journal: Lipids in health and disease20110101

Title: Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport.

Journal: Journal of lipid research20101201

Title: Lack of clinically relevant drug-drug interactions when dalcetrapib is co-administered with ezetimibe.

Journal: British journal of clinical pharmacology20101201

Title: Good news for 'good' cholesterol.

Journal: Nature20101118

Title: Coadministration of dalcetrapib with pravastatin, rosuvastatin, or simvastatin: no clinically relevant drug-drug interactions.

Journal: Journal of clinical pharmacology20101001

Title: No clinically relevant drug-drug interactions when dalcetrapib is co-administered with atorvastatin.

Journal: Expert opinion on investigational drugs20101001

Title: Emerging drugs for hyperlipidemia.

Journal: Expert opinion on emerging drugs20100901

Title: Biochemical characterization of cholesteryl ester transfer protein inhibitors.

Journal: Journal of lipid research20100901

Title: Mechanisms underlying off-target effects of the cholesteryl ester transfer protein inhibitor torcetrapib involve L-type calcium channels.

Journal: Journal of hypertension20100801

Title: Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing.

Journal: European journal of clinical pharmacology20100801

Title: Is a blood pressure rise the only deleterious off-target effect of cholesterol ester transfer protein inhibitors?

Journal: Journal of hypertension20100801

Title: Dissociating HDL cholesterol from cardiovascular risk.

Journal: Lancet (London, England)20100731

Title: Dalcetrapib: a review of Phase II data.

Journal: Expert opinion on investigational drugs20100601

Title: High-density lipoprotein-mediated anti-atherosclerotic and endothelial-protective effects: a potential novel therapeutic target in cardiovascular disease.

Journal: Current pharmaceutical design20100501

Title: Dalcetrapib: JTT 705; JTT-705; R 1658; R1658; RG1658; RO 4607381; RO4607381.

Journal: Drugs in R&D20100501

Title: MARCO, a macrophage scavenger receptor highly expressed in rodents, mediates dalcetrapib-induced uptake of lipids by rat and mouse macrophages.

Journal: Toxicology in vitro : an international journal published in association with BIBRA20100401

Title: [HDL and CETP in atherogenesis].

Journal: Deutsche medizinische Wochenschrift (1946)20100201

Title: Functional assessment of HDL: Moving beyond static measures for risk assessment.

Journal: Cardiovascular drugs and therapy20100201

Title: Safety and tolerability of dalcetrapib (RO4607381/JTT-705): results from a 48-week trial.

Journal: European heart journal20100201

Title: Mulling over the odds of CETP inhibition.

Journal: European heart journal20100201

Title: Cholesteryl ester transfer protein: at the heart of the action of lipid-modulating therapy with statins, fibrates, niacin, and cholesteryl ester transfer protein inhibitors.

Journal: European heart journal20100101

Title: Insights from recent meta-analysis: role of high-density lipoprotein cholesterol in reducing cardiovascular events and rates of atherosclerotic disease progression.

Journal: Journal of clinical lipidology20100101

Title: Update on CETP inhibition.

Journal: Journal of clinical lipidology20100101

Title: Low high-density lipoprotein cholesterol: current status and future strategies for management.

Journal: Vascular health and risk management20100101

Title: High density lipoproteins-based therapies for cardiovascular disease.

Journal: Journal of cardiovascular disease research20100101

Title: Dalcetrapib: no off-target toxicity on blood pressure or on genes related to the renin-angiotensin-aldosterone system in rats.

Journal: British journal of pharmacology20091201

Title: Rationale and design of the dal-OUTCOMES trial: efficacy and safety of dalcetrapib in patients with recent acute coronary syndrome.

Journal: American heart journal20091201

Title: The pharmacology and off-target effects of some cholesterol ester transfer protein inhibitors.

Journal: The American journal of cardiology20091116

Title: Mechanism of inhibition defines CETP activity: a mathematical model for CETP in vitro.

Journal: Journal of lipid research20091101

Title: Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents.

Journal: Expert opinion on therapeutic patents20090901

Title: Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis.

Journal: Current opinion in investigational drugs (London, England : 2000)20090901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology20090901

Title: Free thiol group of MD-2 as the target for inhibition of the lipopolysaccharide-induced cell activation.

Journal: The Journal of biological chemistry20090717

Title: The end of the road for CETP inhibitors after torcetrapib?

Journal: Current opinion in cardiology20090701

Title: Safety and tolerability of dalcetrapib.

Journal: The American journal of cardiology20090701

Title: In vitro and in vivo assessment of the effect of dalcetrapib on a panel of CYP substrates.

Journal: Current medical research and opinion20090401

Title: A single-center, open-label, one-sequence study of dalcetrapib coadministered with ketoconazole, and an in vitro study of the S-methyl metabolite of dalcetrapib.

Journal: Clinical therapeutics20090301

Title: Cholesterylestertransfer protein inhibition and endothelial function in type II hyperlipidemia.

Journal: Thrombosis research20090101

Title: JTT-705: is there still future for a CETP inhibitor after torcetrapib?

Journal: Expert opinion on investigational drugs20081001

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology20080501

Title: Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended?

Journal: Expert opinion on investigational drugs20080401

Title: Is raising HDL a futile strategy for atheroprotection?

Journal: Nature reviews. Drug discovery20080201

Title: HDL metabolism and CETP inhibition.

Journal: Cardiology in review20080101

Title: Gateways to clinical trials. July-August 2008.

Journal: Methods and findings in experimental and clinical pharmacology20080101

Title: The role of CETP inhibition in dyslipidemia.

Journal: Current atherosclerosis reports20070801

Title: The biology and chemistry of hyperlipidemia.

Journal: Bioorganic & medicinal chemistry20070715

Title: Cholesteryl ester transfer protein promotes the formation of cholesterol-rich remnant like lipoprotein particles in human plasma.

Journal: Clinica chimica acta; international journal of clinical chemistry20070101

Title: Inhibition of CETP as a novel therapeutic strategy for reducing the risk of atherosclerotic disease.

Journal: European heart journal20070101

Title: Therapeutic elevation of HDL-cholesterol to prevent atherosclerosis and coronary heart disease.

Journal: Pharmacology & therapeutics20060901

Title: Cholesteryl ester transfer protein inhibition, high-density lipoprotein metabolism and heart disease risk reduction.

Journal: Current opinion in lipidology20060801

Title: Are human CETP mutations and CETP-inhibiting drugs a good or a bad deal?

Journal: Journal of molecular medicine (Berlin, Germany)20060801

Title: Raising high-density lipoprotein with cholesteryl ester transfer protein inhibitors.

Journal: Current opinion in pharmacology20060401

Title: Targeting cholesteryl ester transfer protein for the prevention and management of cardiovascular disease.

Journal: Journal of the American College of Cardiology20060207

Title: Increasing high-density lipoprotein cholesterol through cholesteryl Ester transfer protein inhibition: a next step in the fight against cardiovascular disease?

Journal: Current drug targets. Cardiovascular & haematological disorders20051201

Title: JTT-705 blocks cell proliferation and angiogenesis through p38 kinase/p27(kip1) and Ras/p21(waf1) pathways.

Journal: Atherosclerosis20051001

Title: Consequences of cholesteryl ester transfer protein inhibition in patients with familial hypoalphalipoproteinemia.

Journal: Arteriosclerosis, thrombosis, and vascular biology20050901

Title: Pharmacologic augmentation of high-density lipoproteins: mechanisms of currently available and emerging therapies.

Journal: Current opinion in cardiology20050701

Title: Effectiveness of inhibition of cholesteryl ester transfer protein by JTT-705 in combination with pravastatin in type II dyslipidemia.

Journal: The American journal of cardiology20050501

Title: Role of CETP inhibitors in the treatment of dyslipidemia.

Journal: Current opinion in lipidology20041201

Title: Inhibition of cholesteryl ester transfer protein activity by JTT-705 increases apolipoprotein E-containing high-density lipoprotein and favorably affects the function and enzyme composition of high-density lipoprotein in rabbits.

Journal: Arteriosclerosis, thrombosis, and vascular biology20041001

Title: S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.

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Title: Inhibition of cholesteryl ester transfer protein increases serum apolipoprotein (apo) A-I levels by increasing the synthesis of apo A-I in rabbits.

Journal: Atherosclerosis20040201

Title: Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells.

Journal: American journal of physiology. Endocrinology and metabolism20030601

Title: Effect of JTT-705 on cholesteryl ester transfer protein and plasma lipid levels in normolipidemic animals.

Journal: European journal of pharmacology20030411

Title: Cholesteryl ester transfer protein: a novel target for raising HDL and inhibiting atherosclerosis.

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Title: Cholesteryl ester transfer protein inhibitor (JTT-705) and the development of atherosclerosis in rabbits with severe hypercholesterolaemia.

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Title: The Yin and Yang of cholesteryl ester transfer protein and atherosclerosis.

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Title: Efficacy and safety of a novel cholesteryl ester transfer protein inhibitor, JTT-705, in humans: a randomized phase II dose-response study.

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