Cat. No. 2870
Chemical Name: 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid
Biological ActivityOrally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Anderson et al (2005) Reductions in β-amyloid concentrations in vivo by the γ-secretase inhibitors BMS-289948 and BMS-299897. Biochem.Pharmacol. 69 689. PMID: 15670587.
Barten et al (2005) Dynamics of β-Amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor. J.Pharmacol.Exp.Ther. 312 635. PMID: 15452193.
Goldstein et al (2007) Ex vivo occupancy of the γ-secretase inhibitors correlates with brain β-amyloid peptide reduction in Tg2576 mice. J.Pharmacol.Exp.Ther. 323 102. PMID: 17640949.
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Keywords: BMS 299897, supplier, BMS299897, gamma, secretase, inhibits, orally, active, inhibitors, g-secretase, beta-amyloid, b-amyloid, γ-secretase, β-amyloid
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October 15, 2013