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BMS-708163 (Avagacestat) --- γ-Secretase Inhibitor

Overview
Catalog # bs-60032c-2-mg-solid
Product Name BMS-708163 (Avagacestat) --- γ-Secretase Inhibitor
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 520.88

Formula: C20 H17 Cl F4 N4 O4 S

CAS Number: 1146699-66-2

InChi Key: XEAOPVUAMONVLA-QGZVFWFLSA-N

InChi: InChI=1S/C20H17ClF4N4O4S/c21-14-3-5-15(6-4-14)34(31,32)29(17(18(26)30)7-8-20(23,24)25)10-13-2-1-12(9-16(13)22)19-27-11-33-28-19/h1-6,9,11,17H,7-8,10H2,(H2,26,30)/t17-/m1/s1

Smiles: NC(=O)[C@@H](CCC(F)(F)F)N(CC1C=CC(=CC=1F)C1=NOC=N1)S(=O)(=O)C1C=CC(Cl)=CC=1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description BMS-708163 (Avagacestat) is a potent, selective and orally bioavailable γ-secretase inhibitor with an IC50 of 0.3 nM for APP cleavage. It is 190-fold more selective for APP than Notch, having an IC50 of 58 nM for Notch. Phase I clinical trial studies showed that in humans, BMS-708163 decreased CSF Aβ40 and Aβ42 approximately 30% following daily dose of 100 mg after 28 days and by 60% at daily dose of 150 mg.