Dihydroergocristine mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

二氢麦角新碱甲磺酸盐(DHEC mesylate)是二氢麦角新碱的甲磺酸盐。

Dihydroergocristine 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. 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.(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.

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. 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. Western Blot Analysis Cell Line:WT HEK293 cells; Fibroblast cells Concentration:2 μM, 5 μM, 10 μM, 20 μMIncubation Time:24 hours Result:Increased APP-CTFs accumulation in a dose-dependent manner.

——

DHEC (mesylate)

Membrane Transporter/Ion Channel

Beta Amyloid

CNS

——

——

24730-10-7

707.84

C36H45N5O8S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (70.64 mM)

CS(O)(=O)=O.CC(C)[C@@]1(NC(=O)[C@@H]2C[C@H]3[C@@H](Cc4c[nH]c5cccc3c45)N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O

——

(-20℃)

With Ice Pack

≥ 2 years