Semagacestat(LY450139),γ-分泌酶假抑制剂

Semagacestat (LY450139) (订货以英文为准)

编号:S125519
CAS号:425386-60-3
分子式:C19H27N3O4
分子量:361.44
货号 品牌 包装 目录价 您的价格 库存 数量 购买
S125519-10mg 阿拉丁 10mg ¥729.90
S125519-50mg 阿拉丁 50mg ¥2471.90
S125519-5mg 阿拉丁 5mg ¥395.90
产品名称 Semagacestat (LY450139)
中文名称 Semagacestat(LY450139),γ-分泌酶假抑制剂
CAS号 425386-60-3
分子式(M.F.) C19H27N3O4
分子量(M.W.) 361.44
储存条件 -20°C储存
溶解性≥72 mg/mL in DMSO <1 mg/mL in DMSO ≥43 mg/mL in Ethanol
存贮条件储存温度-20°C
应用A γ-secretase blocker of Aβ42, Aβ40 and Aβ38
产品介绍Semagacestat (LY450139)是一种γ-分泌酶抑制剂,作用于Aβ42, Aβ40和Aβ38时,IC50分别为10.9 nM, 12.1 nM和12.0 nM,也抑制Notch信号通路,IC50为14.1 nM。
备注Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM. Phase 3.
生化机理Semagacestat is an inhibitor of the γ-secretase complex. It causes a reduction in the secretion of Aβ42, Aβ40 and Aβ38 from H4 human glioma cells stably overexpressing human wild-type APP into the culture medium. Semagacestat increases β-CTF in cell lysates, and the increase can be attenuated at high concentrations. Semagacestat inhibits Notch signaling with IC50 of 14.1 nM, and shows minimal Notch-sparing selectivity with Notch IC50/Aβ42 IC50 only 1.3. Semagacestat causes a concentration-dependent decrease in Aβ40 secreted into the medium with IC50 of 111 nM from murine CTX expressing endogenous murine APP, but murine Aβ42 formation in CTX is roughly 12-fold less than Aβ40 in accordance with data for neurons from wild type mice.
别名司马西特; (2S)-2-羟基-3-甲基-N-[(1S)-1-甲基-2-氧代-2-[[(1S)-2,3,4,5-四氢-3-甲基-2-氧代-1H-3-苯并氮杂卓-1-基]氨基]乙基]丁酰胺;LY450139;LY-450139;LY 450139;(2S)-2-Hydroxy-3-methyl-N-[(1S)-1-methyl-2-oxo-2-[[(1S)-2,3,4,5-tetrahydro-3-methyl-2-oxo-1H-3-benzazepin-1-yl]amino]ethyl]butanamide
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