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BMS 299897

Cat. No. 2870

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Chemical Name: 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid

Biological Activity

Orally 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.

Technical Data

M.Wt:

511.94

Formula:

C₂₄H₂₁ClF₃NO₄S

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

>98 %

Storage:

Store at -20°C

CAS No:

290315-45-6

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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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