Name | Dihydroergocristine mesylate |
Description | 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. |
Cell Research | 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]. |
In vitro | The IC50 value(2-20 μM; 24 hours) of Dihydroergocristine (DHEC) for inhibiting the activity of γ-secretase in T100 cells without affecting cell viability is 25 μM.
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 60 mg/mL (84.76 mM), Sonication is recommended. H2O : 1 mg/mL (1.41 mM), Sonication is recommended.
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Keywords | 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 |
Inhibitors Related | Anle138b | BSBM7 | Notoginsenoside R1 | Geniposide | Deferoxamine Mesylate | Tramiprosate | PQM130 | Rutin | EUK-134 | Ginsenoside Rg2 | Methyl tridecanoate | Ginsenoside Re |
Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Neuronal Signaling Compound Library | Anti-Alzheimer's Disease Compound Library | Natural Product Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Natural Product Library for HTS | Bioactive Compounds Library Max |