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.
CAS Number: 1146699-66-2
Molecular Weight: 520.88
Chemical Name: (R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
BMS-708163 was used at 1-10 µM in vitro.
BMS-708163 was dosed orally in female rats at 10 and 100 mg/kg once per day, and could significantly reduced both plasma and brain Aβ40 levels relative to control for the entire dosing interval.
- BMS-708163 was dosed orally in female rats at 10 and 100 mg/kg once per day, and could significantly reduced both plasma and brain Aβ40 levels relative to control for the entire dosing interval.
- Mitani Y, et al. Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. (2012) J Neurosci. 32(6):2037-50.
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