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主营类目:SR1分子,干细胞化合物、实验仪器、试剂、生长因子等
℡ 4000-520-616
℡ 4000-520-616
Cellagen/Categories/5 mg (10 mM solution in DMSO)/C2708-5
产品编号:C2708-5
市  场 价:¥3380.00
场      地:美国(厂家直采)
产品分类: 蛋白类>聚合物>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$169.00
品      牌: Cellagen
公      司:Cellagen Technology LLC
公司分类:
Cellagen/Categories/5 mg (10 mM solution in DMSO)/C2708-5
商品介绍

BMS-708163 (Avagacestat) is a potent and selective inhibitor for gamma-secretase, especially at inhibiting cleavage of amyloid precursor protein (APP) to form amyloid-ß (Aß)(1-40) (IC50=0.3nM) and Aß(1-42) (0.27nM). BMS-708163 is ??Notch sparing??, with more than 100 folds more selective for APP than for Notch protein (IC50 of 58nM). BMS-708163 is developed for treating Alzheimer??s disease (AD). Oral administration of BMS-708163 significantly reduced Aß(1-40) levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs [1]. The results of Phase II clinical trial in mild-to-moderate AD patients demonstrated acceptable tolerability at a single-dose range of 0.3 to 800 mg with a biphasic effect on plasma Aß(1-40) [2].


Technical information:

Chemical Formula:C20H17ClF4N4O4S
CAS #:1146699-66-2
Molecular Weight:520.88
Purity:>98%
Appearance:White
Chemical Name:(2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide
Solubility:Up to 50 mM in DMSO
Synonyms:BMS-708163, BMS 708163, BMS708163, Avagacestat

Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1.Gillman, KW., et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable ?-Secretase Inhibitor. ACS Med. Chem. Lett., 2010, 1 (3): 120??124
2.Tong G., et al., Multicenter, randomized, double-blind, placebo-controlled, single-ascending dose study of the oral ?-secretase inhibitor BMS-708163 (Avagacestat): tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers. Clin Ther. 2012 . 34(3):654-67. Pubmed ID:22381714

Other Information:

Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.

品牌介绍

Cellagen利用广泛的研究以及我们在干细胞生物学,药物化学和产品开发方面的专业知识,Cellagen长期以来一直为专业OEM产品提供世界领先的公司,为一线干细胞研究奠定了基础。

现在,Cellagen扩展了其最佳产品系列,并直接向研究界提供。Cellagen与世界领先的科学家有着密切的联系,并且始终认识到高标准科学研究的未满足需求。


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