| 名称 | Dihydroergocristine mesylate |
| 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. |
| 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]. |
| 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]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 60 mg/mL (84.76 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (2.83 mM), Sonication is recommended.
H2O : 1 mg/mL (1.41 mM), Sonication is recommended.
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| 关键字 | β-amyloid peptide | βAmyloid | β Amyloid | Inhibitor | inhibit | Dihydroergocristine Mesylate | Dihydroergocristine mesylate | Dihydroergocristine | DHEC | BetaAmyloid | Beta Amyloid | bAmyloid | b Amyloid | amyloid-β | Amyloid-β | Abeta |
| 相关产品 | Rutin | Methyl tridecanoate | Ginsenoside Rg2 | Ginsenoside Rg1 | Notoginsenoside R1 | EUK-134 | Tramiprosate | PQM130 | Deferoxamine Mesylate | Anle138b | Geniposide | Ginsenoside Re |
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