BMS 299897

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Cat.No. 2870 - BMS 299897 | C24H21ClF3NO4S | CAS No. 290315-45-6
Description: Potent γ-secretase inhibitor
Chemical Name: 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid
Purity: ≥98% (HPLC)

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 290315-45-6
PubChem ID 11249248
Smiles FC1=CC=[C@@]([C@H](N(C3=CC(F)=CC=C3F)S(C2=CC=C(Cl)C=C2)(=O)=O)C)C(CCCC(O)=O)=C1

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 51.19 100
ethanol 51.19 100

Preparing Stock Solutions

The following data is based on the product molecular weight 511.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.95 mL 9.77 mL 19.53 mL
5 mM 0.39 mL 1.95 mL 3.91 mL
10 mM 0.2 mL 0.98 mL 1.95 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet


References are publications that support the products' biological activity.

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

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

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

If you know of a relevant reference for BMS 299897, please let us know.

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