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Dihydroergocristine mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dihydroergocristine mesylate图片
CAS NO:24730-10-7
包装:100mg
市场价:1607元

产品介绍
Dihydroergocristine mesylate (DHEC mesylate) 是 γ-secretase (GSI) 的抑制剂,减少阿尔茨海默病淀粉样蛋白-β 肽的产生,直接与 γ-secretase 和 Nicastrin 结合,平衡解离常数 (Kd) 为 25.7 nM 和 9.8 μM ,分别。
Cas No.24730-10-7
别名甲磺酸双氢麦角汀,DHEC mesylate
化学名(6aS,9S,10aS)-N-((2S,5S,10aS,10bR)-5-benzyl-10b-hydroxy-2-isopropyl-3,6-dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate
Canonical SMILESOS(=O)(C)=O.O[C@@]1(N(C2=O)[C@@H](CC3=CC=CC=C3)C(N4[C@H]1CCC4)=O)O[C@]2(C(C)C)NC([C@H]5C[C@@H]6[C@H](CC7=CNC8=CC=CC6=C78)N(C)C5)=O
分子式C35H41N5O5.CH3SO3H
分子量707.84
溶解度<17.7mg/ml in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively[1].

Dihydroergocristine (DHEC) (2-20 μM; 24 hours) has an IC50 value of 25 μM for inhibiting the activity of γ-secretase in T100 cells without affecting cell viability[1]. Dihydroergocristine (2-20 μM; 24 hours) inhibits cellular Aβ production and causes a dose-dependent accumulation of carboxy-terminal fragments of APP (APP-CTFs) in HEK293 and decreases γ-secretase activity in fibroblast cells[1].

References:
[1]. Lei X, et al. The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-β peptides. Sci Rep. 2015 Nov 16;5:16541.