Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 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 * 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 | 甲磺酸双氢麦角汀, DHEC (mesylate) |
分子量 | 707.84 |
分子式 | C36H45N5O8S |
CAS No. | 24730-10-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (84.76 mM), Sonication is recommended.
H2O: 1 mg/mL (1.41 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 1.4127 mL | 7.0637 mL | 14.1275 mL | 35.3187 mL |
DMSO | 5 mM | 0.2825 mL | 1.4127 mL | 2.8255 mL | 7.0637 mL |
10 mM | 0.1413 mL | 0.7064 mL | 1.4127 mL | 3.5319 mL | |
20 mM | 0.0706 mL | 0.3532 mL | 0.7064 mL | 1.7659 mL | |
50 mM | 0.0283 mL | 0.1413 mL | 0.2825 mL | 0.7064 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dihydroergocristine mesylate 24730-10-7 Neuroscience Beta Amyloid DHEC β-amyloid peptide Amyloid-β Abeta Dihydroergocristine Dihydroergocristine Mesylate 甲磺酸双氢麦角汀 inhibit DHEC (mesylate) Inhibitor inhibitor