BMS-708163 (Avagacestat), γ-Secretase Inhibitor

Catalog No. size PriceQuantity
M60032-2D 10 mM in DMSO (0.385 mL) $89
M60032-2S 2 mg solid $89
M60032-10S 10 mg solid $365


Product Information
Chemical Name: (R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide
Molecular Weight: 520.89
Formula: C20H17ClF4N4O4S
Purity: ≥ 98%
CAS#: 1146699-66-2
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year


Biological Activity:

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.

How to Use:

In vitro:  BMS-708163 was used at 1-10 µM in vitro.

In vivo: 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.


  1. Gillman K, et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. (2010) ACS Med. Chem. Lett., 1 (3), pp 120–124
  2. 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.

Products are for research use only. Not for human use.

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