Dihydroergocristine mesylate

Research use only, not for human use.

Dihydroergocristine mesylate(DHEC mesylate) is the methanesulfonic acid salt of dihydroergocristine.

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.

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DHEC (mesylate)

Membrane Transporter/Ion Channel

Beta Amyloid

CNS

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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

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(-20℃)

With Ice Pack

≥ 2 years