Home GPCR & G Protein Prostaglandin Receptor chemical Ethamsylate

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Ethamsylate Prostaglandin Receptor chemical

Cat.No.S4152

Ethamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion.
Ethamsylate Prostaglandin Receptor chemical Chemical Structure

Chemical Structure

Molecular Weight: 263.31

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Quality Control

Batch: S415201 DMSO]53 mg/mL]false]Water]53 mg/mL]false]Ethanol]Insoluble]false Purity: 99.91%
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99.91

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (201.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 53 mg/mL

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 263.31 Formula

C6H6O5S.C4H11N

 Storage (From the date of receipt)
CAS No. 2624-44-4 Download SDF Storage of Stock Solutions

Synonyms Etamsylate Smiles CCNCC.C1=CC(=C(C=C1O)S(=O)(=O)O)O

Mechanism of Action

Targets/IC50/Ki
prostaglandins
In vitro
Ethamsylate inhibits prostaglandin bio-synthesis in microsomes of pregnant human myometrium with IC50 of 0.5 mM. This compound is particularly active against hydroxyl radicals (OH.), which are scavenged at therapeutic concentrations (0.1–10 μM). Higher concentrations are required to scavenge superoxide radicals. It potentiates human platelet aggregation and ATP release induced by arachidonic acid, thromboxane A2, collagen, and calcium ionophore A23187.
In vivo
Ethamsylate reduces the mean bleeding time when administered systemically or orally to rabbits. By the intravenous route, this compound reduces bleeding time by half at doses >5 mg/kg. The effect starts 5 minutes after the injection, reaches a maximum between 30 minutes and 4 hours after the injection, and disappears after 6 hours. By the oral route, a similar maximal action is observed at the dose of 10 mg/kg. The efficacy of this chemical to reduce intraventricular hemorrhage is associated with a reduction of thromboxane A2 and prostacyclin biosynthesis. Orally given Ethamsylate (>25 mg/kg) also inhibits carrageenan-induced rat paw edema.
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