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BMS-708163 (Avagacestat) - γ-Secretase Inhibitor. CAS# 1146699-66-2 B-PNP Notch inhibition induces cochlear hair

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Description

Notch inhibition induces cochlear hair cell regeneration and recovery of hearing after acoustic trauma

1 µM final concentration in vitro and in cellular assays

InChi: InChI=1S/C29H44F2N6O2/c1-21(2)36-14-7-22(8-15-36)32-27-23-19-25(38-3)26(39-18-6-13-35-11-4-5-12-35)20-24(23)33-28(34-27)37-16-9-29(30

PMID: 19696185

(2012) Stem Cell Res

BMS-708163 (Avagacestat) - γ-Secretase Inhibitor. CAS# 1146699-66-2 B-PNP Notch inhibition induces cochlear hairBMS 708163 (Avagacestat), CAS No. 1146699 66 2, is a potent, selective and orally bioavailable 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 A40 and A42 approximately 30% following daily dose of 100 mg after 28 days and by 60% at daily dose of 150 mg. Product information CAS

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