BMS 299897

BMS-299897 markedly reduced both brain and plasma Abeta in APP-YAC mice with ED(50) values of 86 and 22 mg/kg per os (po), respectively[1]. BMS 299897 is a selective inhibitor for gamma-secretase. Reductions in the formation of Abeta peptides by gamma-secretase inhibitors may be a viable therapy for reducing Abeta in Alzheimer's disease. BMS-299897 is a gamma-secretase inhibitor that was effective in reducing amyloid beta-peptide (A beta) in transgenic mice and guinea pigs[3]. in vitro: BMS-299897 dose-dependently increased brain concentrations of APP carboxy-terminal fragments, consistent with inhibition of gamma-secretase. BMS-299897 (100 mg/kg po) reduced brain and plasma Abeta(1-40) rapidly (within 20min) and maximally within 3 h. BMS-299897 dose-dependently reduced cortical, cerebrospinal fluid (CSF), and plasma Abeta in guinea pigs with ED(50) values of 30 mg/kg intraperitoneally, without affecting CSF levels of alpha-sAPP. The reductions in cortical Abeta correlated significantly with the reductions in both plasma (r(2) = 0.77) and CSF (r(2) = 0.61) Abeta [1]. in vivo: BMS-299897blocked the Aβ(25-35)-induced deficits in spontaneous alternation or novel object recognition, using a 1h intertrial time interval. BMS-299896 failed to affect the passive avoidance impairments or novel object recognition, using a 24h intertrial time interval [2]. Clinical trial: Study to Evaluate the Safety, Pharmacokinetics and Tolerability of BMS-299897 .Phage I.you can refer to more information at http://www.medchemexpress.com