565793

γ-Secretase Inhibitor XXIV, BMS299897

The γ-Secretase Inhibitor XXIV, BMS299897, also referenced under CAS 290315-45-6, controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

• 别名: γ-Secretase Inhibitor XXIV, BMS299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid, BMS-299897, BMS 299897
• 经验公式（希尔记法）: C₂₄H₂₁ClF₃NO₄S
• CAS号: 290315-45-6
• 分子量: 511.94
• MDL编号: MFCD12963627
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥97% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: white
• 溶解性: ethanol: 100 mM; DMSO: 50 mg/mL
• 运输: ambient
• 储存温度: 2-8°C
• SMILES字符串: FC1=CC(CCCC(O)=O)=C([C@@H](C)N(S(=O)(C2=CC=C(Cl)C=C2)=O)C3=C(F)C=CC(F)=C3)C=C1
• InChI: 1S/C24H21ClF3NO4S/c1-15(21-11-7-18(26)13-16(21)3-2-4-24(30)31)29(23-14-19(27)8-12-22(23)28)34(32,33)20-9-5-17(25)6-10-20/h5-15H,2-4H2,1H3,(H,30,31)/t15-/m1/s1
• InChI key: IZAOBRWCUGOKNH-OAHLLOKOSA-N

说明

一般描述

A cell-permeable sulfonamide compound that preferentially inhibits γ-secretase activity toward APP CTF over Notch-1 (IC₅₀ against APP_SW CTF and murine ΔE-Notch processing = 7.1 and 105.9 nM, respectively, in HEK293) in a presenillin 1-/PS1-selective manner (IC₅₀ = 8 and 308 nM against APP_SW processing in PS1^-/-PS2^-/-MEF expressing human PS1 and PS2, respectively). BMS-299897 is shown to be orally available, readily cross blood-brain-barrier (<15 min), and effectively suppress plasma and brain Aβ level in transgenic mice bearing normal human APP (APP-YAC) or APP_SW/APP_K670N/M671L (Tg2576) in a time- and dose-dependent manner (optimal p.o. dose 100 mg/kg) in vivo. However, BMS-299897 is not effective in reducing Aβ in aged, plaque-bearing murine brain and long-term daily drug dosing is reported to result in increased drug metabolizing activity in mice.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Zhao, B., et al. 2008. J. Biol. Chem. 283, 2927.
Barten, D.M., et al. 2005. J. Pharmacol. Exp. Ther.312, 635.
Anderson, J.J., et al. 2005. Biochem. Pharmacol.69, 689.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable