Catalog No.:AA003U74

654671-78-0 | 1-Butanone, 3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-, (3R)-, phosphate (1:1)

Name: Name:1-Butanone, 3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-, (3R)-, phosphate (1:1)
Brand: AABLOCKS
SKU: AA003U74
Availability: InStock
Rating: 90 (10 reviews)

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Technical Information
Properties
Downstream Synthesis Route
Literature
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Technical Information
Properties
Downstream Synthesis Route
Literature

Technical Information

Catalog Number:

AA003U74

Chemical Name:

1-Butanone, 3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-, (3R)-, phosphate (1:1)

CAS Number:

654671-78-0

Molecular Formula:

C16H18F6N5O5P

Molecular Weight:

505.3088

MDL Number:

MFCD09952339

SMILES:

OP(=O)(O)O.N[C@H](Cc1cc(F)c(cc1F)F)CC(=O)N1CCn2c(C1)nnc2C(F)(F)F

Properties

Form:

Solid

MP:

202-204°C

Storage:

Inert atmosphere;2-8℃;

Computed Properties

Complexity:

616

Covalently-Bonded Unit Count:

Defined Atom Stereocenter Count:

Heavy Atom Count:

Hydrogen Bond Acceptor Count:

Hydrogen Bond Donor Count:

Rotatable Bond Count:

Downstream Synthesis Route

654671-77-9

sitagliptinphosphate

[1]Patent:WO2006/33848,2006,A1.Locationinpatent:Page/Pagecolumn14

[2]Patent:WO2005/30127,2005,A2.Locationinpatent:Page/Pagecolumn13

sitagliptinphosphate

654671-77-9

[1]Patent:US2013/158265,2013,A1

Literature

Title: Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.

Journal: Chemical research in toxicology 20150518

Title: High fat diet and GLP-1 drugs induce pancreatic injury in mice.

Journal: Toxicology and applied pharmacology 20140415

Title: Novel hydrazine derivatives as selective DPP-IV inhibitors: findings from virtual screening and validation through molecular dynamics simulations.

Journal: Journal of molecular modeling 20140401

Title: Oral L-glutamine increases active GLP-1 (7-36) amide secretion and improves glycemic control in stretpozotocin-nicotinamide induced diabetic rats.

Journal: Chemico-biological interactions 20130425

Title: A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations.

Journal: European journal of pharmacology 20121205

Title: Glucagon-like peptide-1 (GLP-1) receptor agonism or DPP-4 inhibition does not accelerate neoplasia in carcinogen treated mice.

Journal: Regulatory peptides 20121110

Title: Quantitative model of the relationship between dipeptidyl peptidase-4 (DPP-4) inhibition and response: meta-analysis of alogliptin, saxagliptin, sitagliptin, and vildagliptin efficacy results.

Journal: Journal of clinical pharmacology 20121001

Title: Patient-reported outcomes in trials of incretin-based therapies in patients with type 2 diabetes mellitus.

Journal: Diabetes, obesity & metabolism 20121001

Title: Effects of saxagliptin and sitagliptin on glycaemic control and pancreatic β-cell mass in a streptozotocin-induced mouse model of type 2 diabetes.

Journal: Diabetes, obesity & metabolism 20121001

Title: No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects.

Journal: Diabetes, obesity & metabolism 20121001

Title: Effects of a combination of sitagliptin plus metformin vs metformin monotherapy on glycemic control, β-cell function and insulin resistance in type 2 diabetic patients.

Journal: Diabetes research and clinical practice 20121001

Title: Reduction of oxidative stress and inflammation by blunting daily acute glucose fluctuations in patients with type 2 diabetes: role of dipeptidyl peptidase-IV inhibition.

Journal: Diabetes care 20121001

Title: Add-on therapies to metformin in type 2 diabetes: what modulates the respective decrements in postprandial and basal glucose?

Journal: Diabetes technology & therapeutics 20121001

Title: Continuous glucose profiles with vildagliptin versus sitagliptin in add-on to metformin: results from the randomized Optima study.

Journal: Diabetes & metabolism 20121001

Title: Dipeptidyl peptidase 4 inhibition increases myocardial glucose uptake in nonischemic cardiomyopathy.

Journal: Journal of cardiac failure 20121001

Title: Pharmacokinetics of empagliflozin, a sodium glucose cotransporter-2 (SGLT-2) inhibitor, coadministered with sitagliptin in healthy volunteers.

Journal: Advances in therapy 20121001

Title: Comparison between sitagliptin as add-on therapy to insulin and insulin dose-increase therapy in uncontrolled Korean type 2 diabetes: CSI study.

Journal: Diabetes, obesity & metabolism 20120901

Title: Combined treatment with a dipeptidyl peptidase-IV inhibitor (sitagliptin) and an angiotensin II type 1 receptor blocker (losartan) promotes islet regeneration via enhanced differentiation of pancreatic progenitor cells.

Journal: Diabetes, obesity & metabolism 20120901

Title: The addition of sitagliptin to ongoing metformin therapy significantly improves glycemic control in Chinese patients with type 2 diabetes.

Journal: Journal of diabetes 20120901

Title: Sitagliptin exerts anti-inflammatory and anti-allergic effects in ovalbumin-induced murine model of allergic airway disease.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20120901

Title: Sitagliptin exerts an antinflammatory action.

Journal: The Journal of clinical endocrinology and metabolism 20120901

Title: Dipeptidyl peptidase IV regulates proliferation of preglomerular vascular smooth muscle and mesangial cells.

Journal: Hypertension (Dallas, Tex. : 1979) 20120901

Title: Dipeptidyl peptidase 4 inhibitor sitagliptin protects endothelial function in hypertension through a glucagon-like peptide 1-dependent mechanism.

Journal: Hypertension (Dallas, Tex. : 1979) 20120901

Title: [Nephropathy and metabolic heart diseases. Cardiac risk in kidney malfunction].

Journal: MMW Fortschritte der Medizin 20120823

Title: Factors predicting therapeutic efficacy of combination treatment with sitagliptin and metformin in type 2 diabetic patients: the COSMETIC study.

Journal: Clinical endocrinology 20120801

Title: Drug eruption caused by sitagliptin, a dipeptidyl peptidase-IV inhibitor.

Journal: The Journal of dermatology 20120801

Title: Efficacy and safety of initial combination therapy with sitagliptin and pioglitazone in patients with type 2 diabetes: a 54-week study.

Journal: Diabetes, obesity & metabolism 20120801

Title: Glycaemic efficacy of glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors as add-on therapy to metformin in subjects with type 2 diabetes-a review and meta analysis.

Journal: Diabetes, obesity & metabolism 20120801

Title: Sitagliptin reduces plaque macrophage content and stabilises arteriosclerotic lesions in Apoe (-/-) mice.

Journal: Diabetologia 20120801

Title: Mechanisms for the antihyperglycemic effect of sitagliptin in patients with type 2 diabetes.

Journal: The Journal of clinical endocrinology and metabolism 20120801

Title: Lower risk of hypoglycemia with sitagliptin compared to glipizide when either is added to metformin therapy: a pre-specified analysis adjusting for the most recently measured HbA(1c) value.

Journal: Current medical research and opinion 20120801

Title: The effects of sitagliptin on gastric emptying in healthy humans - a randomised, controlled study.

Journal: Alimentary pharmacology & therapeutics 20120801

Title: Hypoglycemia in patients with type 2 diabetes from India and Malaysia treated with sitagliptin or a sulfonylurea during Ramadan: a randomized, pragmatic study.

Journal: Current medical research and opinion 20120801

Title: Mechanism of action of DPP-4 inhibitors--new insights.

Journal: The Journal of clinical endocrinology and metabolism 20120801

Title: Exenatide and sitagliptin are not associated with increased risk of acute renal failure: a retrospective claims analysis.

Journal: Diabetes, obesity & metabolism 20120701

Title: Sitagliptin promotes macrophage-to-faeces reverse cholesterol transport through reduced intestinal cholesterol absorption in obese insulin resistant CETP-apoB100 transgenic mice.

Journal: Diabetes, obesity & metabolism 20120701

Title: The effect of sitagliptin versus glibenclamide on arterial stiffness, blood pressure, lipids, and inflammation in type 2 diabetes mellitus patients.

Journal: Diabetes technology & therapeutics 20120701

Title: Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study.

Journal: Current medical research and opinion 20120701

Title: Evaluation of vulvovaginal symptoms and Candida colonization in women with type 2 diabetes mellitus treated with canagliflozin, a sodium glucose co-transporter 2 inhibitor.

Journal: Current medical research and opinion 20120701

Title: [Liraglutide: new results in the treatment of type 2 diabetes mellitus].

Journal: Drugs of today (Barcelona, Spain : 1998) 20120701

Title: Insulin glargine versus sitagliptin in insulin-naive patients with type 2 diabetes mellitus uncontrolled on metformin (EASIE): a multicentre, randomised open-label trial.

Journal: Lancet (London, England) 20120616

Title: Choosing a blood-glucose-lowering agent after metformin.

Journal: Lancet (London, England) 20120616

Title: Combination exenatide-sitagliptin therapy used with glipizide in a patient with type 2 diabetes mellitus.

Journal: American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 20120615

Title: [Efficacy of tianmaixiaoke tablets in the treatment of newly diagnosed type 2 diabetes mellitus in China].

Journal: Zhonghua yi xue za zhi 20120612

Title: Miglitol administered before breakfast increased plasma active glucagon-like peptide-1 (GLP-1) levels after lunch in patients with type 2 diabetes treated with sitagliptin.

Journal: Acta diabetologica 20120601

Title: Saxagliptin and sitagliptin in adult patients with type 2 diabetes: a systematic review and meta-analysis.

Journal: Diabetes, obesity & metabolism 20120601

Title: Pharmacokinetic evaluation of atorvastatin and sitagliptin in combination for the treatment of type 2 diabetes.

Journal: Expert opinion on drug metabolism & toxicology 20120601

Title: Effects of sitagliptin in diabetic patients with nonalcoholic steatohepatitis.

Journal: Acta gastro-enterologica Belgica 20120601

Title: Rhabdomyolysis precipitated by a sitagliptin-atorvastatin drug interaction.

Journal: Diabetic medicine : a journal of the British Diabetic Association 20120501

Title: Initial therapy with the fixed-dose combination of sitagliptin and metformin results in greater improvement in glycaemic control compared with pioglitazone monotherapy in patients with type 2 diabetes.

Journal: Diabetes, obesity & metabolism 20120501

Title: Protective effects of the dipeptidyl peptidase IV inhibitor sitagliptin in the blood-retinal barrier in a type 2 diabetes animal model.

Journal: Diabetes, obesity & metabolism 20120501

Title: Pharmacokinetic drug interaction between gemfibrozil and sitagliptin in healthy Indian male volunteers.

Journal: European journal of clinical pharmacology 20120501

Title: An update in incretin-based therapy: a focus on dipeptidyl peptidase--4 inhibitors.

Journal: Current diabetes reviews 20120501

Title: Sitagliptin add-on to low dosage sulphonylureas: efficacy and safety of combination therapy on glycaemic control and insulin secretion capacity in type 2 diabetes.

Journal: International journal of clinical practice 20120501

Title: Immunotherapies in diabetes mellitus type 1.

Journal: The Medical clinics of North America 20120501

Title: Association between sitagliptin adherence and self-monitoring of blood glucose.

Journal: Journal of diabetes science and technology 20120501

Title: Decreased hepatic glucose production in obese rats by dipeptidyl peptidase-IV inhibitor sitagliptin.

Journal: Chinese medical journal 20120501

Title: The combination of colesevelam with sitagliptin enhances glycemic control in diabetic ZDF rat model.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20120415

Title: DPP-4 inhibitors in the management of type 2 diabetes: a critical review of head-to-head trials.

Journal: Diabetes & metabolism 20120401

Title: Sitagliptin increases tau phosphorylation in the hippocampus of rats with type 2 diabetes and in primary neuron cultures.

Journal: Neurobiology of disease 20120401

Title: The design of the liraglutide clinical trial programme.

Journal: Diabetes, obesity & metabolism 20120401

Title: Cost-utility analysis of liraglutide compared with sulphonylurea or sitagliptin, all as add-on to metformin monotherapy in Type 2 diabetes mellitus.

Journal: Diabetic medicine : a journal of the British Diabetic Association 20120301

Title: Comparing the efficacy and safety profile of sitagliptin versus glimepiride in patients of type 2 diabetes mellitus inadequately controlled with metformin alone.

Journal: The Journal of the Association of Physicians of India 20120301

Title: Upregulation of CD26 expression in epithelial cells and stromal cells during wound-induced skin tumour formation.

Journal: Oncogene 20120223

Title: The importance of green chemistry in process research and development.

Journal: Chemical Society reviews 20120221

Title: Persistent edematous-plaque photosensitivity observed with sitagliptin phosphate (Januvia®).

Journal: Dermatology online journal 20120215

Title: Contributing factors related to efficacy of the dipeptidyl peptidase-4 inhibitor sitagliptin in Japanese patients with type 2 diabetes.

Journal: Diabetes research and clinical practice 20120201

Title: Dipeptidyl peptidase IV (DPPIV/CD26) inhibition does not improve engraftment of unfractionated syngeneic or allogeneic bone marrow after nonmyeloablative conditioning.

Journal: Experimental hematology 20120201

Title: Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue.

Journal: Endocrinology 20120201

Title: Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug-naive patients with type 2 diabetes (DURATION-4): a 26-week double-blind study.

Journal: Diabetes care 20120201

Title: Psoriasiform eruption triggered by a dipeptidyl peptidase IV inhibitor.

Journal: The Australasian journal of dermatology 20120201

Title: A dipeptidyl peptidase-4 inhibitor, des-fluoro-sitagliptin, improves endothelial function and reduces atherosclerotic lesion formation in apolipoprotein E-deficient mice.

Journal: Journal of the American College of Cardiology 20120117

Title: Dipeptidyl peptidase-4 inhibitor: another player for cardiovascular protection.

Journal: Journal of the American College of Cardiology 20120117

Title: Evaluation of Modification of Diet in Renal Disease Study and Cockcroft-Gault equations for sitagliptin dosing.

Journal: Journal of nephrology 20120101

Title: Dipeptidyl peptidase IV inhibition improves cardiorenal function in overpacing-induced heart failure.

Journal: European journal of heart failure 20120101

Title: Effect of initial combination therapy with sitagliptin and metformin on β-cell function in patients with type 2 diabetes.

Journal: Diabetes, obesity & metabolism 20120101

Title: The safety, efficacy and predictors for HbA1c reduction of sitagliptin in the treatment of Japanese type 2 diabetes.

Journal: Diabetes research and clinical practice 20120101

Title: Sitagliptin, a dipeptidyl peptidase-IV inhibitor, improves psoriasis.

Journal: Dermatology (Basel, Switzerland) 20120101

Title: Case report of acute necrotizing pancreatitis associated with combination treatment of sitagliptin and exenatide.

Journal: Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists 20120101

Title: Why do metabolites circulate?

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20120101

Title: Serum level of soluble CD26/dipeptidyl peptidase-4 (DPP-4) predicts the response to sitagliptin, a DPP-4 inhibitor, in patients with type 2 diabetes controlled inadequately by metformin and/or sulfonylurea.

Journal: Translational research : the journal of laboratory and clinical medicine 20120101

Title: Non-alcoholic fatty liver disease adversely affects the glycemic control afforded by sitagliptin.

Journal: Hepato-gastroenterology 20120101

Title: Long-term efficacy of sitagliptin for the treatment of type 2 diabetic patients in Japan.

Journal: Endocrine journal 20120101

Title: [The new antidiabetic agents in the firing line.... safety reasons or witch hunt?].

Journal: Endocrinologia y nutricion : organo de la Sociedad Espanola de Endocrinologia y Nutricion 20120101

Title: Suicide attempt by an overdose of sitagliptin, an oral hypoglycemic agent: a case report and a review of the literature.

Journal: Endocrine journal 20120101

Title: Sitagliptin in glutamic acid decarboxylase antibody-positive diabetes mellitus.

Journal: Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists 20120101

Title: Long-term cost-consequence analysis of exenatide once weekly vs sitagliptin or pioglitazone for the treatment of type 2 diabetes patients in the United States.

Journal: Journal of medical economics 20120101

Title: Intentional weight loss and dose reductions of anti-diabetic medications--a retrospective cohort study.

Journal: PloS one 20120101

Title: Reversible mitral and aortic regurgitation due to pioglitazone.

Journal: Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists 20120101

Title: Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor.

Journal: BMC pharmacology 20120101

Title: Effect of a dipeptidyl peptidase-IV inhibitor, des-fluoro-sitagliptin, on neointimal formation after balloon injury in rats.

Journal: PloS one 20120101

Title: Hypoglycemics for the treatment of type 2 diabetes in patients with chronic kidney disease: a focus on new agents.

Journal: CANNT journal = Journal ACITN 20120101

Title: A new preventive strategy for hypoglycemia incorporating added food diet in patients with type 2 diabetes who received sitagliptin therapy.

Journal: Endocrine research 20120101

Title: Long-term clinical and economic outcomes associated with liraglutide versus sitagliptin therapy when added to metformin in the treatment of type 2 diabetes: a CORE Diabetes Model analysis.

Journal: Journal of medical economics 20120101

Title: Sitagliptin (DPP-4 inhibitor)-induced rheumatoid arthritis in type 2 diabetes mellitus: a case report.

Journal: Internal medicine (Tokyo, Japan) 20120101

Title: Comparison of vildagliptin twice daily vs. sitagliptin once daily using continuous glucose monitoring (CGM): crossover pilot study (J-VICTORIA study).

Journal: Cardiovascular diabetology 20120101

Title: The effectiveness of liraglutide in nonalcoholic fatty liver disease patients with type 2 diabetes mellitus compared to sitagliptin and pioglitazone.

Journal: TheScientificWorldJournal 20120101

Title: Combination of mangiferin and dipeptidyl peptidase-4 inhibitor sitagliptin improves impaired glucose tolerance in streptozotocin-diabetic rats.

Journal: Pharmacology 20120101

Title: The effects of simvastatin on the pharmacokinectics of sitagliptin.

Journal: Journal of population therapeutics and clinical pharmacology = Journal de la therapeutique des populations et de la pharamcologie clinique 20120101

Title: Effects of DPP-4 inhibition on cardiac metabolism and function in mice.

Journal: Journal of molecular and cellular cardiology 20111201

Title: Sitagliptin therapy in kidney transplant recipients with new-onset diabetes after transplantation.

Journal: Transplantation 20111127

Title: [Incretin-based therapy for treating patients with type 2 diabetes].

Journal: Orvosi hetilap 20111127

Title: Sitagliptin and simvastatin (juvisync).

Journal: The Medical letter on drugs and therapeutics 20111114

Title: Effects of exenatide twice daily versus sitagliptin on 24-h glucose, glucoregulatory and hormonal measures: a randomized, double-blind, crossover study.

Journal: Diabetes, obesity & metabolism 20111101

Title: Encapsulation of exenatide in poly-(D,L-lactide-co-glycolide) microspheres produced an investigational long-acting once-weekly formulation for type 2 diabetes.

Journal: Diabetes technology & therapeutics 20111101

Title: Effect of sitagliptin monotherapy on serum total ghrelin levels in people with type 2 diabetes.

Journal: Diabetes research and clinical practice 20111101

Title: Target-mediated metabolism and target-mediated drug disposition of the DPPIV inhibitor AMG 222.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20111101

Title: The incidence of hypoglycaemia in Muslim patients with type 2 diabetes treated with sitagliptin or a sulphonylurea during Ramadan: a randomised trial.

Journal: International journal of clinical practice 20111101

Title: Exenatide and sitagliptin: pancreatitis and pancreatic cancer. Harms on the rise.

Journal: Prescrire international 20111101

Title: Both sitagliptin analogue & pioglitazone preserve the beta-cell proportion in the islets with different mechanism in non-obese and obese diabetic mice.

Journal: BMB reports 20111101

Title: [Sitagliptin in the treatment of type 2 diabetes: new data presented during the American Diabetes Association annual meeting (San Diego, California, June 2011)].

Journal: Drugs of today (Barcelona, Spain : 1998) 20111101

Title: Effect of sitagliptin on glucose control in adult patients with Type 1 diabetes: a pilot, double-blind, randomized, crossover trial.

Journal: Diabetic medicine : a journal of the British Diabetic Association 20111001

Title: Evaluation of the interaction between sitagliptin and cyclodextrin derivatives by capillary electrophoresis and nuclear magnetic resonance spectroscopy.

Journal: Electrophoresis 20111001

Title: [Dipeptidyl-peptidase-4 inhibitors (gliptins): a new class of oral antidiabetic drugs].

Journal: Orvosi hetilap 20110911

Title: Sitagliptin, a dipeptidyl peptidase-4 inhibitor, does not affect the pharmacokinetics of ethinyl estradiol or norethindrone in healthy female subjects.

Journal: Journal of clinical pharmacology 20110901

Title: Sitagliptin or exenatide once weekly for type 2 diabetes: comparison of the clinical trials.

Journal: Expert opinion on pharmacotherapy 20110901

Title: A treatment strategy implementing combination therapy with sitagliptin and metformin results in superior glycaemic control versus metformin monotherapy due to a low rate of addition of antihyperglycaemic agents.

Journal: Diabetes, obesity & metabolism 20110901

Title: The metabolic syndrome influences the response to incretin-based therapies.

Journal: Acta diabetologica 20110901

Title: Efficacy and safety of sitagliptin and the fixed-dose combination of sitagliptin and metformin vs. pioglitazone in drug-naïve patients with type 2 diabetes.

Journal: International journal of clinical practice 20110901

Title: Sitagliptin augments protective effects of GLP-1 against advanced glycation end product receptor axis in endothelial cells.

Journal: Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme 20110901

Title: Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?

Journal: Journal of medicinal chemistry 20110825

Title: Development of a molecularly imprinted polymer for selective extraction followed by liquid chromatographic determination of sitagliptin in rat plasma and urine.

Journal: Talanta 20110815

Title: Merging the best of two worlds: artificial metalloenzymes for enantioselective catalysis.

Journal: Chemical communications (Cambridge, England) 20110814

Title: Inhibition of anaphylaxis like reaction and mast cell activation by Sitagliptin.

Journal: International immunopharmacology 20110801

Title: DPP-IV inhibitor may affect spermatogenesis.

Journal: Diabetes research and clinical practice 20110801

Title: Physiological and pharmacological mechanisms through which the DPP-4 inhibitor sitagliptin regulates glycemia in mice.

Journal: Endocrinology 20110801

Title: Improved outcome of islet transplantation in partially pancreatectomized diabetic mice by inhibition of dipeptidyl peptidase-4 with sitagliptin.

Journal: Pancreas 20110801

Title: Protective effects of dipeptidyl peptidase-4 (DPP-4) inhibitor against increased β cell apoptosis induced by dietary sucrose and linoleic acid in mice with diabetes.

Journal: The Journal of biological chemistry 20110722

Title: Liquid chromatographic determination of sitagliptin either alone or in ternary mixture with metformin and sitagliptin degradation product.

Journal: Talanta 20110715

Title: Pancreatitis, pancreatic, and thyroid cancer with glucagon-like peptide-1-based therapies.

Journal: Gastroenterology 20110701

Title: The effect of initial therapy with the fixed-dose combination of sitagliptin and metformin compared with metformin monotherapy in patients with type 2 diabetes mellitus.

Journal: Diabetes, obesity & metabolism 20110701

Title: Sitagliptin more effectively achieves a composite endpoint for A1C reduction, lack of hypoglycemia and no body weight gain compared with glipizide.

Journal: Diabetes research and clinical practice 20110701

Title: Effects of sitagliptin on 24-h glycemic changes in Japanese patients with type 2 diabetes assessed using continuous glucose monitoring.

Journal: Diabetes technology & therapeutics 20110701

Title: Pancreatic ultrastructural enhancement due to telmisartan plus sitagliptin treatment in diet-induced obese C57BL/6 mice.

Journal: Pancreas 20110701

Title: Sitagliptin: a review.

Journal: Expert opinion on pharmacotherapy 20110701

Title: GLP-1-based therapies: the dilemma of uncertainty.

Journal: Gastroenterology 20110701

Title: Efficacy and safety of long-acting glucagon-like peptide-1 receptor agonists compared with exenatide twice daily and sitagliptin in type 2 diabetes mellitus: a systematic review and meta-analysis.

Journal: The Annals of pharmacotherapy 20110701

Title: Renal impairment with sitagliptin: is there a need for active monitoring of potential renal toxicity?

Journal: British journal of hospital medicine (London, England : 2005) 20110701

Title: DURATION-2: efficacy and safety of switching from maximum daily sitagliptin or pioglitazone to once-weekly exenatide.

Journal: Diabetic medicine : a journal of the British Diabetic Association 20110601

Title: Simultaneous quantitation of metformin and sitagliptin from mouse and human dried blood spots using laser diode thermal desorption tandem mass spectrometry.

Journal: Journal of pharmaceutical and biomedical analysis 20110601

Title: Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin in older adults with type 2 diabetes mellitus.

Journal: Journal of the American Geriatrics Society 20110601

Title: Successful long-term use of sitagliptin for the treatment of new-onset diabetes mellitus after solid organ transplantation: a case report.

Journal: Transplantation proceedings 20110601

Title: [Determination of sitagliptin phosphate in rat plasma by ultra high performance liquid chromatography-tandem mass spectrometry].

Journal: Se pu = Chinese journal of chromatography 20110601

Title: An analysis of the impact of FDA's guidelines for addressing cardiovascular risk of drugs for type 2 diabetes on clinical development.

Journal: Contemporary clinical trials 20110501

Title: Effect of sitagliptin plus metformin on β-cell function, islet integrity and islet gene expression in Zucker diabetic fatty rats.

Journal: Diabetes research and clinical practice 20110501

Title: Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial.

Journal: Current medical research and opinion 20110501

Title: [Incretin enhancer: sitagliptin].

Journal: Nihon rinsho. Japanese journal of clinical medicine 20110501

Title: Journal withdraws article after complaints from drug manufacturers.

Journal: BMJ (Clinical research ed.) 20110411

Title: Effect of sitagliptin therapy on postprandial lipoprotein levels in patients with type 2 diabetes.

Journal: Diabetes, obesity & metabolism 20110401

Title: One year of liraglutide treatment offers sustained and more effective glycaemic control and weight reduction compared with sitagliptin, both in combination with metformin, in patients with type 2 diabetes: a randomised, parallel-group, open-label trial.

Journal: International journal of clinical practice 20110401

Title: [Efficacy and tolerability of sitagliptin in type 2 diabetic patients inadequately controlled with metformin. A prospective observational study in austrian primary care].

Journal: Wiener klinische Wochenschrift 20110401

Title: Dipeptidyl peptidase IV inhibition attenuates blood pressure rising in young spontaneously hypertensive rats.

Journal: Journal of hypertension 20110301

Title: Expression and spatial heterogeneity of dipeptidyl peptidases in endothelial cells of conduct vessels and capillaries.

Journal: Biological chemistry 20110301

Title: Substance P-induced skin inflammation is not modulated by a single dose of sitagliptin in human volunteers.

Journal: Biological chemistry 20110301

Title: Efficacy and safety of insulin detemir once daily in combination with sitagliptin and metformin: the TRANSITION randomized controlled trial.

Journal: Diabetes, obesity & metabolism 20110301

Title: Evaluation of pharmacokinetic parameters and dipeptidyl peptidase-4 inhibition following single doses of sitagliptin in healthy, young Japanese males.

Journal: British journal of clinical pharmacology 20110301

Title: Sitagliptin and metformin--novel combination therapy.

Journal: Expert opinion on pharmacotherapy 20110301

Title: Liraglutide improves treatment satisfaction in people with Type 2 diabetes compared with sitagliptin, each as an add on to metformin.

Journal: Diabetic medicine : a journal of the British Diabetic Association 20110301

Title: Sitagliptin lowers glucagon and improves glucose tolerance in prediabetic obese SHROB rats.

Journal: Experimental biology and medicine (Maywood, N.J.) 20110301

Title: A diabetes drug, sitagliptin, also has a potential to prevent diabetes.

Journal: Experimental biology and medicine (Maywood, N.J.) 20110301

Title: Sitagliptin manufacture: a compelling tale of green chemistry, process intensification, and industrial asymmetric catalysis.

Journal: Angewandte Chemie (International ed. in English) 20110225

Title: Sitagliptin/metformin fixed-dose combination: in patients with type 2 diabetes mellitus.

Journal: Drugs 20110212

Title: Severe leucopenia associated with Sitagliptin use.

Journal: Diabetes research and clinical practice 20110201

Title: Dipeptidyl peptidase IV inhibitor sitagliptin reduces local inflammation in adipose tissue and in pancreatic islets of obese mice.

Journal: American journal of physiology. Endocrinology and metabolism 20110201

Title: Differential effects of PPAR-{gamma} activation versus chemical or genetic reduction of DPP-4 activity on bone quality in mice.

Journal: Endocrinology 20110201

Title: Efficacy and safety of treatment with sitagliptin or glimepiride in patients with type 2 diabetes inadequately controlled on metformin monotherapy: a randomized, double-blind, non-inferiority trial.

Journal: Diabetes, obesity & metabolism 20110201

Title: Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and pioglitazone on glycemic control and measures of β-cell function in patients with type 2 diabetes.

Journal: International journal of clinical practice 20110201

Title: Weight-related quality of life, health utility, psychological well-being, and satisfaction with exenatide once weekly compared with sitagliptin or pioglitazone after 26 weeks of treatment.

Journal: Diabetes care 20110201

Title: Sitagliptin, a dipeptidyl peptidase-4 inhibitor, decreases systolic blood pressure in Japanese hypertensive patients with type 2 diabetes.

Journal: The Tohoku journal of experimental medicine 20110201

Title: Pharmacology of GLP-1 agonists: describing the therapeutic potential to patients.

Journal: The Journal of the American Osteopathic Association 20110201

Title: Incretin therapies in the management of elderly patients with type 2 diabetes mellitus.

Journal: Hospital practice (1995) 20110201

Title: Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Journal: Journal of medicinal chemistry 20110127

Title: Sitagliptin protects renal ischemia reperfusion induced renal damage in diabetes.

Journal: Regulatory peptides 20110117

Title: Sitagliptin prevents the development of metabolic and hormonal disturbances, increased β-cell apoptosis and liver steatosis induced by a fructose-rich diet in normal rats.

Journal: Clinical science (London, England : 1979) 20110101

Title: Lack of pharmacokinetic interaction between dapagliflozin, a novel sodium-glucose transporter 2 inhibitor, and metformin, pioglitazone, glimepiride or sitagliptin in healthy subjects.

Journal: Diabetes, obesity & metabolism 20110101

Title: Effectiveness of sitagliptin in asian Indian patients with type 2 diabetes-an Indian tertiary diabetes care center experience.

Journal: Diabetes technology & therapeutics 20110101

Title: Sitagliptin reduces albuminuria in patients with type 2 diabetes.

Journal: Endocrine journal 20110101

Title: Focus on incretin-based therapies: targeting the core defects of type 2 diabetes.

Journal: Postgraduate medicine 20110101

Title: A case of drug-induced hepatic injury associated with sitagliptin.

Journal: Internal medicine (Tokyo, Japan) 20110101

Title: Sitagliptin compared with thiazolidinediones as a third-line oral antihyperglycemic agent in type 2 diabetes mellitus.

Journal: Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists 20110101

Title: Comparative efficacy of vildagliptin and sitagliptin in Japanese patients with type 2 diabetes mellitus: a matching-adjusted indirect comparison of randomized trials.

Journal: Clinical drug investigation 20110101

Title: [Glycemic control before and after sitagliptin in general medical practice: analysis of determinant factors in the Belgian observational study 'SUGAR'].

Journal: Revue medicale de Liege 20110101

Title: Sitagliptin as a novel treatment agent for non-alcoholic Fatty liver disease patients with type 2 diabetes mellitus.

Journal: Hepato-gastroenterology 20110101

Title: Effects of DPP-4 inhibitors on the heart in a rat model of uremic cardiomyopathy.

Journal: PloS one 20110101

Title: A pilot study of the efficacy of miglitol and sitagliptin for type 2 diabetes with a continuous glucose monitoring system and incretin-related markers.

Journal: Cardiovascular diabetology 20110101

Title: Diabetic nephropathy amelioration by a low-dose sitagliptin in an animal model of type 2 diabetes (Zucker diabetic fatty rat).

Journal: Experimental diabetes research 20110101

Title: Sitagliptin attenuates metformin-mediated AMPK phosphorylation through inhibition of organic cation transporters.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20101201

Title: [Hypoglycemia in the diabetes treatment - risk minimization with dipeptidyl peptidase-4 inhibitors].

Journal: Drugs of today (Barcelona, Spain : 1998) 20101201

Title: Safety and efficacy of SITAgliptin plus GRanulocyte-colony-stimulating factor in patients suffering from Acute Myocardial Infarction (SITAGRAMI-Trial)--rationale, design and first interim analysis.

Journal: International journal of cardiology 20101119

Title: Acute pancreatitis in type 2 diabetes treated with exenatide or sitagliptin: a retrospective observational pharmacy claims analysis.

Journal: Diabetes care 20101101

Title: DPP-4 inhibitors: what may be the clinical differentiators?

Journal: Diabetes research and clinical practice 20101101

Title: Characteristics of patients prescribed sitagliptin and other oral antihyperglycaemic agents in a large US claims database.

Journal: International journal of clinical practice 20101101

Title: [New data from the US-American Diabetes Congress. GLP-1 effect: more than reducing blood glucose].

Journal: MMW Fortschritte der Medizin 20101007

Title: Dipeptidyl peptidase IV inhibition alters the hemodynamic response to angiotensin-converting enzyme inhibition in humans with the metabolic syndrome.

Journal: Hypertension (Dallas, Tex. : 1979) 20101001

Title: Interactive hemodynamic effects of dipeptidyl peptidase-IV inhibition and angiotensin-converting enzyme inhibition in humans.

Journal: Hypertension (Dallas, Tex. : 1979) 20101001

Title: Pharmacokinetic and pharmacodynamic evaluation of sitagliptin plus metformin.

Journal: Expert opinion on drug metabolism & toxicology 20101001

Title: Incretin action maintains insulin secretion, but not hepatic insulin action, in people with impaired fasting glucose.

Journal: Diabetes research and clinical practice 20101001

Title: Efficacy and safety of saxagliptin in combination with metformin compared with sitagliptin in combination with metformin in adult patients with type 2 diabetes mellitus.

Journal: Diabetes/metabolism research and reviews 20101001

Title: Initial short-term intensive insulin therapy as a strategy for evaluating the preservation of beta-cell function with oral antidiabetic medications: a pilot study with sitagliptin.

Journal: Diabetes, obesity & metabolism 20101001

Title: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions.

Journal: Clinical pharmacokinetics 20100901

Title: Distinguishing among incretin-based therapies. Glucose-lowering effects of incretin-based therapies.