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BMS 299897
Cat No.
CEI-1249
Description
BMS 299897 is a potent and orally active inhibitor of γ-secretase with IC50 value of 12 nM.
Product Overview
BMS-299897 is a selective inhibitor of γ-secretase with IC50 value of 12 nM. γ-secretase is an intergral membrane protein whose well-known substrate is amyloid precursor protein and involves in the process of cleaving single-pass transmembrane proteins at residues with the transmembrane domain. It has been revealed thatγ-secretase cleave APP in any of multiple sites and generate a 39 to 42 amino acids long peptide, among which Aβ40 is the most common isoform and Aβ42 is the most susceptible to conformational changes leading to amyloid fibrillogenesis. Many studies have shown that reduction of brain Aβ synthesis by gamma-secretase inhibitors is a promising approach for the Alzheimers disease treatment. BMS 299897 is a selective inhibitorγ-secretase. When tested HEKwt culture with BMS-299897, the expression of Aβ(1-40) in culture supernatant had a robust rise throughγ-secretase inhibition. In male Swiss mice model with intracerebroventricular (i. c. v.) injection of Aβ(25-35) which induced Alzheimers disease pathomimetic toxicity, administration of BMS-299897 markedly attenuated Aβ(1-42)-whose accumulation marginally contributed to the toxicity or long-term memory deficits-seeding and toxicity induced by Aβ(25-35) through inhibiting γ-secretase. When tested with Tg2576 mice, oral administration of BMS-299897 markedly reduced Abeta peptide concentrations by inhibitingγ-secretase.
CAS No.
290315-45-6
Molecular Weight
511.94
Purity
0.98
Storage
Store at -20°C
Targets
γ-secretase
IC50
12 nM
Molecular Formula
C24H21ClF3NO4S
Chemical Name
4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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