425386-60-3 Usage
Description
Semagacestat is a pharmaceutical compound that functions as an inhibitor of the γ-secretase enzyme, which plays a crucial role in the production of β-amyloid (Aβ), a neurotoxic peptide associated with the pathogenesis of Alzheimer's disease (AD). It is characterized by its white solid chemical properties.
Uses
Used in Pharmaceutical Industry:
Semagacestat is used as an inhibitor for the γ-secretase enzyme to target the reduction of β-amyloid (Aβ) peptide generation, which is implicated in the development of Alzheimer's disease (AD). By inhibiting this enzyme, Semagacestat aims to slow down or halt the progression of the disease, offering a potential therapeutic approach for patients suffering from AD.
Biological Activity
semagacestat (also known as ly450139), [(2s)-2-hydroxy-n-((2s)-1-((1s)-3-methyl-2-oxo-2,3,4,5-tetrahydro-1h-benzo[d]azepin-1ylamino)-1-oxopropan-2-yl)-3-methylbutanamide] is an azepine class γ-secretase, which is currently being investigated as a potential disease-modifying agent for the treatment of alzheimer’s disease (ad). it reduces the rate of formation of amyloid-β (aβ), a major component of the neuritic plaque in the brains of ad patients, in human subjects and animal models including mice, beagle dogs and guinea pigs. according to previous studies, semagacestat slows the accumulation of aβ in the brains of transgenic mice overexpressing mutant human amyloid precursor protein v717f (pdapp mice) and exhibits a dose-dependent decrease of plasma in ad patients.ping yi, chad hadden, palaniappan kulanthaivel, nathan calvert, william annes, thomas brown, robert j. barbuch, archana chaudhary, mosun a. ayan-oshodi, and barbara j. ring. disposition and metabolism of semagacestat, a γ-secretase inhibitor, in humans. drug metabolism and disposition 2010; 38(4): 554-565
Check Digit Verification of cas no
The CAS Registry Mumber 425386-60-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,2,5,3,8 and 6 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 425386-60:
(8*4)+(7*2)+(6*5)+(5*3)+(4*8)+(3*6)+(2*6)+(1*0)=153
153 % 10 = 3
So 425386-60-3 is a valid CAS Registry Number.
InChI:InChI=1/C19H27N3O4/c1-11(2)16(23)18(25)20-12(3)17(24)21-15-14-8-6-5-7-13(14)9-10-22(4)19(15)26/h5-8,11-12,15-16,23H,9-10H2,1-4H3,(H,20,25)(H,21,24)/t12-,15-,16-/m0/s1
425386-60-3Relevant articles and documents
Synthesis of a substituted benzazepin-2-one dihydrate
Boini, Sathish K.,Vaid, Radhe K.,Moder, Kenneth P.,Mitchell, David
experimental part, p. 1983 - 1986 (2010/01/13)
Synthesis of the title compound was accomplished via coupling of (S)-alaninyl-(S)-1-amino-3-methyl-4,5,6,7-tetrahydro-2H-3-benzazepin-2-one with the activated trimethylsilyl ester of (S)-2-trimethylsilyloxy-3-methylbutyric acid, followed by deprotection a
