209984-57-6,MFCD09832551
Catalog No.:AA002KFF

209984-57-6 | Ly411575

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98%
in stock  
$45.00   $31.00
- +
5mg
98%
in stock  
$128.00   $90.00
- +
10mg
98%
in stock  
$219.00   $154.00
- +
25mg
98%
in stock  
$373.00   $261.00
- +
  • Technical Information
  • Properties
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA002KFF
Chemical Name:
Ly411575
CAS Number:
209984-57-6
Molecular Formula:
C26H23F2N3O4
Molecular Weight:
479.4753
MDL Number:
MFCD09832551
SMILES:
Fc1cc(F)cc(c1)[C@@H](C(=O)N[C@H](C(=O)N[C@H]1c2ccccc2c2c(N(C1=O)C)cccc2)C)O
Properties
Computed Properties
 
Complexity:
789  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
3  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
35  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0  
Rotatable Bond Count:
5  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  
XLogP3:
3  

Literature

Title: A phase 3 trial of semagacestat for treatment of Alzheimer's disease.

Journal: The New England journal of medicine 20130725

Title: Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20121226

Title: The effects on metabolic clearance when administering a potent CYP3A autoinducer with the prototypic CYP3A inhibitor, ketoconazole.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20121001

Title: Semagacestat pharmacokinetics are not significantly affected by formulation, food, or time of dosing in healthy participants.

Journal: Journal of clinical pharmacology 20120601

Title: miR-9 controls the timing of neurogenesis through the direct inhibition of antagonistic factors.

Journal: Developmental cell 20120515

Title: A brain aggregate model gives new insights into the pathobiology and treatment of prion diseases.

Journal: Journal of neuropathology and experimental neurology 20120501

Title: First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms.

Journal: The Journal of biological chemistry 20120406

Title: Γ-secretase modulators do not induce Aβ-rebound and accumulation of β-C-terminal fragment.

Journal: Journal of neurochemistry 20120401

Title: QT effect of semagacestat at therapeutic and supratherapeutic doses.

Journal: International journal of clinical pharmacology and therapeutics 20120401

Title: Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20120208

Title: A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

Journal: Journal of Alzheimer's disease : JAD 20120101

Title: Evaluation of the performance of novel Aβ isoforms as theragnostic markers in Alzheimer's disease: from the cell to the patient.

Journal: Neuro-degenerative diseases 20120101

Title: Translatability scoring in drug development: eight case studies.

Journal: Journal of translational medicine 20120101

Title: Advances in the identification of γ-secretase inhibitors for the treatment of Alzheimer's disease.

Journal: Expert opinion on drug discovery 20120101

Title: Modulation of γ-secretase activity by multiple enzyme-substrate interactions: implications in pathogenesis of Alzheimer's disease.

Journal: PloS one 20120101

Title: Amyloid-β(1-15/16) as a marker for γ-secretase inhibition in Alzheimer's disease.

Journal: Journal of Alzheimer's disease : JAD 20120101

Title: γ-Secretase modulator in Alzheimer's disease: shifting the end.

Journal: Journal of Alzheimer's disease : JAD 20120101

Title: pPKCα-mediated effect on in vitro Aβ production in response to gamma secretase inhibitor LY411575 in rat CTXTNA2 astrocytes.

Journal: Journal of biological regulators and homeostatic agents 20120101

Title: Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.

Journal: The Journal of pharmacology and experimental therapeutics 20111201

Title: [Gamma-secretase inhibitors and modulators].

Journal: Nihon rinsho. Japanese journal of clinical medicine 20111201

Title: Drugs: a tangled web of targets.

Journal: Nature 20110713

Title: Prevalence of asymptomatic vasogenic edema in pretreatment Alzheimer's disease study cohorts from phase 3 trials of semagacestat and solanezumab.

Journal: Alzheimer's & dementia : the journal of the Alzheimer's Association 20110701

Title: What the halted phase III γ-secretase inhibitor trial may (or may not) be telling us.

Journal: Annals of neurology 20110201

Title: New pathway links γ-secretase to inflammation and memory while sparing notch.

Journal: Annals of neurology 20110101

Title: Validation of ELISA methods for quantification of total tau and phosporylated-tau181 in human cerebrospinal fluid with measurement in specimens from two Alzheimer's disease studies.

Journal: Journal of Alzheimer's disease : JAD 20110101

Title: BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells.

Journal: Journal of biomedical science 20110101

Title: Interacting with γ-secretase for treating Alzheimer's disease: from inhibition to modulation.

Journal: Current medicinal chemistry 20110101

Title: Genetics. Gamma-secretase and human disease.

Journal: Science (New York, N.Y.) 20101119

Title: What can be inferred from the interruption of the semagacestat trial for treatment of Alzheimer's disease?

Journal: Biological psychiatry 20101115

Title: Alzheimer's failure raises questions about disease-modifying strategies.

Journal: Nature reviews. Drug discovery 20101001

Title: NerveCenter: Phase III Alzheimer trial halted: Search for therapeutic biomarkers continues.

Journal: Annals of neurology 20101001

Title: ACS chemical neuroscience molecule spotlight on semagacestat (LY450139).

Journal: ACS chemical neuroscience 20100818

Title: [Progress in the development of anti-amyloid drugs for treatment of Alzheimer's disease.].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20100701

Title: Disposition and metabolism of semagacestat, a {gamma}-secretase inhibitor, in humans.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20100401

Title: In response to 'a gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system'.

Journal: Annals of neurology 20100101

Title: Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.

Journal: Journal of Alzheimer's disease : JAD 20100101

Title: Use of theragnostic markers to select drugs for phase II/III trials for Alzheimer disease.

Journal: Alzheimer's research & therapy 20100101

Title: Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Journal: Alzheimer's research & therapy 20100101

Title: Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.

Journal: Journal of medicinal chemistry 20091022

Title: Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo.

Journal: Journal of neurochemistry 20090901

Title: A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system.

Journal: Annals of neurology 20090701

Title: Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease.

Journal: Expert opinion on pharmacotherapy 20090701

Title: Semagacestat, a gamma-secretase inhibitor for the potential treatment of Alzheimer's disease.

Journal: Current opinion in investigational drugs (London, England : 2000) 20090701

Title: gamma-Secretase inhibitor reduces diet-induced atherosclerosis in apolipoprotein E-deficient mice.

Journal: Biochemical and biophysical research communications 20090529

Title: Committed neuronal precursors confer astrocytic potential on residual neural precursor cells.

Journal: Developmental cell 20090201

Title: Requirement of Notch activation during regeneration of the intestinal epithelia.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20090101

Title: A small molecule inhibitor of signal peptide peptidase inhibits Plasmodium development in the liver and decreases malaria severity.

Journal: PloS one 20090101

Title: Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575.

Journal: Molecular neurodegeneration 20090101

Title: Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.

Journal: The Journal of pharmacology and experimental therapeutics 20081101

Title: Notch1 and TGFbeta1 cooperatively regulate Foxp3 expression and the maintenance of peripheral regulatory T cells.

Journal: Blood 20080901

Title: Molecule of the month. Semagacestat.

Journal: Drug news & perspectives 20080901

Title: Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease.

Journal: Archives of neurology 20080801

Title: A multigram chemical synthesis of the gamma-secretase inhibitor LY411575 and its diastereoisomers.

Journal: Bioorganic & medicinal chemistry letters 20071115

Title: Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase.

Journal: The Journal of biological chemistry 20071102

Title: Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20071101

Title: Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.

Journal: The Journal of biological chemistry 20070824

Title: Dominance of amyloid precursor protein sequence over host cell secretases in determining beta-amyloid profiles studies of interspecies variation and drug action by internally standardized immunoprecipitation/mass spectrometry.

Journal: The Journal of pharmacology and experimental therapeutics 20070301

Title: Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase.

Journal: Clinical neuropharmacology 20070101

Title: Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse.

Journal: The Journal of pharmacology and experimental therapeutics 20061201

Title: Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.

Journal: The Journal of pharmacology and experimental therapeutics 20061101

Title: [The molecular mechanism of Notch-induced transformation and the therapeutic potential of its inhibitor].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20060701

Title: Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease.

Journal: Neurology 20060227

Title: Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].

Journal: The Journal of pharmacology and experimental therapeutics 20050501

Title: Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers.

Journal: Clinical neuropharmacology 20050101

Title: Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY-411575).

Journal: The Journal of pharmacology and experimental therapeutics 20040401

Title: Wong GT, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82.

Title: Otoguro T, et al. Inhibitory effect of presenilin inhibitor LY411575 on maturation of hepatitis C virus core protein, production of the viral particle and expression of host proteins involved in pathogenicity. Microbiol Immunol. 2016 Nov;60(11):740-753

Title: Curry CL, et al. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in Kaposi's sarcoma tumor cells. Oncogene. 2005 Sep 22;24(42):6333-44.

Title: Zhang J, et al. Notch signaling modulates proliferative vitreoretinopathy via regulating retinal pigment epithelial-to-mesenchymal transition. Histochem Cell Biol. 2017 Mar;147(3):367-375.

Title: Hyde LA, et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,dazepin-7-yl-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther. 2006 Dec;319(3):1133-43.

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Tags:209984-57-6 Molecular Formula|209984-57-6 MDL|209984-57-6 SMILES|209984-57-6 Ly411575
Catalog No.: AA002KFF
209984-57-6,MFCD09832551
209984-57-6 | Ly411575
Pack Size: 1mg
Purity: 98%
in stock
$45.00 $31.00
Pack Size: 5mg
Purity: 98%
in stock
$128.00 $90.00
Pack Size: 10mg
Purity: 98%
in stock
$219.00 $154.00
Pack Size: 25mg
Purity: 98%
in stock
$373.00 $261.00
Quantity
- +
Add to Card
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bulk Quotation Request
Technical Information
Catalog Number: AA002KFF
Chemical Name: Ly411575
CAS Number: 209984-57-6
Molecular Formula: C26H23F2N3O4
Molecular Weight: 479.4753
MDL Number: MFCD09832551
SMILES: Fc1cc(F)cc(c1)[C@@H](C(=O)N[C@H](C(=O)N[C@H]1c2ccccc2c2c(N(C1=O)C)cccc2)C)O
Properties
Complexity: 789  
Covalently-Bonded Unit Count: 1  
Defined Atom Stereocenter Count: 3  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 35  
Hydrogen Bond Acceptor Count: 6  
Hydrogen Bond Donor Count: 3  
Isotope Atom Count: 0  
Rotatable Bond Count: 5  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
XLogP3: 3  
Literature fold

Title: A phase 3 trial of semagacestat for treatment of Alzheimer's disease.

Journal: The New England journal of medicine20130725

Title: Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design.

Journal: Proceedings of the National Academy of Sciences of the United States of America20121226

Title: The effects on metabolic clearance when administering a potent CYP3A autoinducer with the prototypic CYP3A inhibitor, ketoconazole.

Journal: Drug metabolism and disposition: the biological fate of chemicals20121001

Title: Semagacestat pharmacokinetics are not significantly affected by formulation, food, or time of dosing in healthy participants.

Journal: Journal of clinical pharmacology20120601

Title: miR-9 controls the timing of neurogenesis through the direct inhibition of antagonistic factors.

Journal: Developmental cell20120515

Title: A brain aggregate model gives new insights into the pathobiology and treatment of prion diseases.

Journal: Journal of neuropathology and experimental neurology20120501

Title: First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms.

Journal: The Journal of biological chemistry20120406

Title: Γ-secretase modulators do not induce Aβ-rebound and accumulation of β-C-terminal fragment.

Journal: Journal of neurochemistry20120401

Title: QT effect of semagacestat at therapeutic and supratherapeutic doses.

Journal: International journal of clinical pharmacology and therapeutics20120401

Title: Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience20120208

Title: A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

Journal: Journal of Alzheimer's disease : JAD20120101

Title: Evaluation of the performance of novel Aβ isoforms as theragnostic markers in Alzheimer's disease: from the cell to the patient.

Journal: Neuro-degenerative diseases20120101

Title: Translatability scoring in drug development: eight case studies.

Journal: Journal of translational medicine20120101

Title: Advances in the identification of γ-secretase inhibitors for the treatment of Alzheimer's disease.

Journal: Expert opinion on drug discovery20120101

Title: Modulation of γ-secretase activity by multiple enzyme-substrate interactions: implications in pathogenesis of Alzheimer's disease.

Journal: PloS one20120101

Title: Amyloid-β(1-15/16) as a marker for γ-secretase inhibition in Alzheimer's disease.

Journal: Journal of Alzheimer's disease : JAD20120101

Title: γ-Secretase modulator in Alzheimer's disease: shifting the end.

Journal: Journal of Alzheimer's disease : JAD20120101

Title: pPKCα-mediated effect on in vitro Aβ production in response to gamma secretase inhibitor LY411575 in rat CTXTNA2 astrocytes.

Journal: Journal of biological regulators and homeostatic agents20120101

Title: Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.

Journal: The Journal of pharmacology and experimental therapeutics20111201

Title: [Gamma-secretase inhibitors and modulators].

Journal: Nihon rinsho. Japanese journal of clinical medicine20111201

Title: Drugs: a tangled web of targets.

Journal: Nature20110713

Title: Prevalence of asymptomatic vasogenic edema in pretreatment Alzheimer's disease study cohorts from phase 3 trials of semagacestat and solanezumab.

Journal: Alzheimer's & dementia : the journal of the Alzheimer's Association20110701

Title: What the halted phase III γ-secretase inhibitor trial may (or may not) be telling us.

Journal: Annals of neurology20110201

Title: New pathway links γ-secretase to inflammation and memory while sparing notch.

Journal: Annals of neurology20110101

Title: Validation of ELISA methods for quantification of total tau and phosporylated-tau181 in human cerebrospinal fluid with measurement in specimens from two Alzheimer's disease studies.

Journal: Journal of Alzheimer's disease : JAD20110101

Title: BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells.

Journal: Journal of biomedical science20110101

Title: Interacting with γ-secretase for treating Alzheimer's disease: from inhibition to modulation.

Journal: Current medicinal chemistry20110101

Title: Genetics. Gamma-secretase and human disease.

Journal: Science (New York, N.Y.)20101119

Title: What can be inferred from the interruption of the semagacestat trial for treatment of Alzheimer's disease?

Journal: Biological psychiatry20101115

Title: Alzheimer's failure raises questions about disease-modifying strategies.

Journal: Nature reviews. Drug discovery20101001

Title: NerveCenter: Phase III Alzheimer trial halted: Search for therapeutic biomarkers continues.

Journal: Annals of neurology20101001

Title: ACS chemical neuroscience molecule spotlight on semagacestat (LY450139).

Journal: ACS chemical neuroscience20100818

Title: [Progress in the development of anti-amyloid drugs for treatment of Alzheimer's disease.].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica20100701

Title: Disposition and metabolism of semagacestat, a {gamma}-secretase inhibitor, in humans.

Journal: Drug metabolism and disposition: the biological fate of chemicals20100401

Title: In response to 'a gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system'.

Journal: Annals of neurology20100101

Title: Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.

Journal: Journal of Alzheimer's disease : JAD20100101

Title: Use of theragnostic markers to select drugs for phase II/III trials for Alzheimer disease.

Journal: Alzheimer's research & therapy20100101

Title: Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Journal: Alzheimer's research & therapy20100101

Title: Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.

Journal: Journal of medicinal chemistry20091022

Title: Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo.

Journal: Journal of neurochemistry20090901

Title: A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system.

Journal: Annals of neurology20090701

Title: Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease.

Journal: Expert opinion on pharmacotherapy20090701

Title: Semagacestat, a gamma-secretase inhibitor for the potential treatment of Alzheimer's disease.

Journal: Current opinion in investigational drugs (London, England : 2000)20090701

Title: gamma-Secretase inhibitor reduces diet-induced atherosclerosis in apolipoprotein E-deficient mice.

Journal: Biochemical and biophysical research communications20090529

Title: Committed neuronal precursors confer astrocytic potential on residual neural precursor cells.

Journal: Developmental cell20090201

Title: Requirement of Notch activation during regeneration of the intestinal epithelia.

Journal: American journal of physiology. Gastrointestinal and liver physiology20090101

Title: A small molecule inhibitor of signal peptide peptidase inhibits Plasmodium development in the liver and decreases malaria severity.

Journal: PloS one20090101

Title: Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575.

Journal: Molecular neurodegeneration20090101

Title: Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.

Journal: The Journal of pharmacology and experimental therapeutics20081101

Title: Notch1 and TGFbeta1 cooperatively regulate Foxp3 expression and the maintenance of peripheral regulatory T cells.

Journal: Blood20080901

Title: Molecule of the month. Semagacestat.

Journal: Drug news & perspectives20080901

Title: Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease.

Journal: Archives of neurology20080801

Title: A multigram chemical synthesis of the gamma-secretase inhibitor LY411575 and its diastereoisomers.

Journal: Bioorganic & medicinal chemistry letters20071115

Title: Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase.

Journal: The Journal of biological chemistry20071102

Title: Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.

Journal: Bioorganic & medicinal chemistry letters20071101

Title: Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.

Journal: The Journal of biological chemistry20070824

Title: Dominance of amyloid precursor protein sequence over host cell secretases in determining beta-amyloid profiles studies of interspecies variation and drug action by internally standardized immunoprecipitation/mass spectrometry.

Journal: The Journal of pharmacology and experimental therapeutics20070301

Title: Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase.

Journal: Clinical neuropharmacology20070101

Title: Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse.

Journal: The Journal of pharmacology and experimental therapeutics20061201

Title: Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.

Journal: The Journal of pharmacology and experimental therapeutics20061101

Title: [The molecular mechanism of Notch-induced transformation and the therapeutic potential of its inhibitor].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology20060701

Title: Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease.

Journal: Neurology20060227

Title: Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].

Journal: The Journal of pharmacology and experimental therapeutics20050501

Title: Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers.

Journal: Clinical neuropharmacology20050101

Title: Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY-411575).

Journal: The Journal of pharmacology and experimental therapeutics20040401

Title: Wong GT, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82.

Title: Otoguro T, et al. Inhibitory effect of presenilin inhibitor LY411575 on maturation of hepatitis C virus core protein, production of the viral particle and expression of host proteins involved in pathogenicity. Microbiol Immunol. 2016 Nov;60(11):740-753

Title: Curry CL, et al. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in Kaposi's sarcoma tumor cells. Oncogene. 2005 Sep 22;24(42):6333-44.

Title: Zhang J, et al. Notch signaling modulates proliferative vitreoretinopathy via regulating retinal pigment epithelial-to-mesenchymal transition. Histochem Cell Biol. 2017 Mar;147(3):367-375.

Title: Hyde LA, et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,dazepin-7-yl-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther. 2006 Dec;319(3):1133-43.

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