BMS-708163(Avagacestat),γ-SecretaseInhibitor

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.

Reference:

1. 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. 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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