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 |
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
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 |
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