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Dihydroergocristine mesylate

Catalog No. T11043   CAS 24730-10-7
Synonyms: DHEC (mesylate)

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.

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Dihydroergocristine mesylate Chemical Structure
Dihydroergocristine mesylate, CAS 24730-10-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 332.00
50 mg In stock $ 495.00
100 mg In stock $ 676.00
1 mL * 10 mM (in DMSO) In stock $ 191.00
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Purity: 99.65%
Purity: 99.51%
Purity: 98.9%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 GSI:25 μM
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].
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].
Synonyms DHEC (mesylate)
Molecular Weight 707.84
Formula C36H45N5O8S
CAS No. 24730-10-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49 mg/mL (69.22 mM), Sonification is recommended.

H2O: 1 mg/mL (1.41 mM)

TargetMolReferences and Literature

1. Lei X, et al. The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-β peptides. Sci Rep. 2015 Nov 16;5:16541.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Anti-Alzheimer's Disease Compound Library Anti-Cardiovascular Disease Compound Library Neuronal Signaling Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Approved Drug Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Dihydroergocristine mesylate 24730-10-7 Neuroscience Beta Amyloid DHEC β-amyloid peptide Amyloid-β Abeta Dihydroergocristine Dihydroergocristine Mesylate inhibit DHEC (mesylate) Inhibitor inhibitor

 

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