产品属性：
产品名称 | 规格 | CAS号 | 型号 |
BMS 299897 | 10mg | 290315-45-6 | EY-Y0163955 |
Cas No.290315-45-6
别名
化学名 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid
分子式 C24H21ClF3NO4S
分子量 511.94
溶解度 Soluble in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
BMS-299897 is a selective inhibitor of γ-secretase with IC50 value of 12 nM [1].
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 Alzheimer's disease treatment [1] [2].
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 [3].
In male Swiss mice model with intracerebroventricular (i.c.v.) injection of Aβ(25-35) which induced Alzheimer's 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 [4]. When tested with Tg2576 mice, oral administration of BMS-299897 markedly reduced Abeta peptide concentrations by inhibitingγ-secretase [5] [2].
References:
[1]. Anderson, J.J., et al., Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897. Biochem Pharmacol, 2005. 69(4): p. 689-98.
[2]. Barten, D.M., et al., Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor. J Pharmacol Exp Ther, 2005. 312(2): p. 635-43.
[3]. Burton, C.R., et al., The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression. J Biol Chem, 2008. 283(34): p. 22992-3003.
[4]. Meunier, J., et al., The gamma-secretase inhibitor 2-[(1R)-1-[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl) amino]ethyl-5-fluorobenzenebutanoic acid (BMS-299897) alleviates Abeta1-42 seeding and short-term memory deficits in the Abeta25-35 mouse model of Alzheimer's disease. Eur J Pharmacol, 2013. 698(1-3): p. 193-9.
[5]. Goldstein, M.E., et al., Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice. J Pharmacol Exp Ther, 2007. 323(1): p. 102-8.
关键字： 290315-45-6;C24H21ClF3NO4S;BMS 299897;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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