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Dihydroergocristine mesylate (DHEC (mesylate)) 是一种 γ-secretase (GSI) 的抑制剂,能够阿尔茨海默氏病淀粉样蛋白 β 肽 (amyloid-β) 的产生,与 γ-secretase 和 Nicastrin 结合的平衡解离常数 (Kd) 值分别为 25.7 nM 和 9.8 μM。
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Dihydroergocristine mesylate (DHEC (mesylate)) 是一种 γ-secretase (GSI) 的抑制剂,能够阿尔茨海默氏病淀粉样蛋白 β 肽 (amyloid-β) 的产生,与 γ-secretase 和 Nicastrin 结合的平衡解离常数 (Kd) 值分别为 25.7 nM 和 9.8 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 492 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,930 | 现货 | |
25 mg | ¥ 3,290 | 现货 | |
50 mg | ¥ 4,610 | 现货 | |
100 mg | ¥ 6,570 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,894 | 现货 |
产品描述 | Dihydroergocristine mesylate (DHEC (mesylate))(DHEC mesylate) is the methanesulfonic acid salt of dihydroergocristine. It has been used as the for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease. Dihydroergocristine 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]. It is also a component of ergoloid mesylate (codergocrine mesilate), a mixture of ergot alkaloid derivatives that is used as a vasodilator and has shown mild benefits in the treatment of vascular dementia. It has a role as a vasodilator agent, an alpha-adrenergic antagonist and a geroprotector. It contains a dihydroergocristine. |
靶点活性 | GSI:25 μM |
体外活性 | Dihydroergocristine (DHEC)在T100细胞中抑制γ-分泌酶活性的IC50值(2-20 μM;24小时)为25 μM,且不影响细胞存活率。在HEK293细胞中,Dihydroergocristine 剂量依赖性地抑制细胞内Aβ产生,诱导APP羧基末端片段(APP-CTFs)的积累,并在成纤维细胞中降低γ-分泌酶活性[1]。 |
细胞实验 | Dihydroergocristine (2-20 μM; 24 hours) causes a dose-dependent accumulation of carboxy-terminal fragments of APP (APP-CTFs) in HEK293 and decreases γ-secretase activity in fibroblast cells and inhibits cellular Aβ production[1]. |
别名 | DHEC (mesylate), 甲磺酸双氢麦角汀 |
分子量 | 707.84 |
分子式 | C36H45N5O8S |
CAS No. | 24730-10-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (84.76 mM), Sonication is recommended. H2O: 1 mg/mL (1.41 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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