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γ-Secretase Inhibitor BMS-708163 (Avagacestat)

Chemical Name:  (R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide

Molecular Weight:

     520.88

Formula:

     C20H17ClF4N4O4S

Purity:

     ≥98%

CAS#:

     1146699-66-2

Solubility:

     DMSO up to 100mM

Storage:

     Powder:  4oC 1 year

     DMSO:  4oC  3 month

                    -20oC 1 year

BMS-708163 (Avagacestat)

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Product Name Catalog No. Amount Price Qty
BMS-708163 (Avagacestat) M60032-2s 2 mg solid
$89.00
BMS-708163 (Avagacestat) M60032-2 10 mM in DMSO (0.385 mL)
$89.00
BMS-708163 (Avagacestat) M60032-b Bulk Request - Bulk Inquiry
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Details


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.

 

Product Specification           Product MSDS

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