A selective 5-HT2 receptor antagonist (Kis = 3.02

Sarpogrelate (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
135159-51-2
Storage:
-20
UN-No:
Non-Hazardous - /

Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).{39654} It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).{39658} In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).{39655} In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.{39656} Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.{39657}  

 

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SKU: 24194 - 250 mg Category:

Description

A selective 5-HT2 receptor antagonist (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant 5-HT2A, 5-HT2B, and 5-HT2C expressed in CHO-K1 cells); selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM); inhibits aggregation of rat whole blood induced by collagen, 5-HT with collagen, and 5-HT with ADP (IC50s = 57.7, 0.56, and 22.7 μM, respectively); inhibits HFFD-induced leukocyte-endothelial interactions in the femoral artery in mice (5 mg/kg per day); decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction (5 mg/kg per day),

Formal name: butanedioic acid, 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester, monohydrochloride

Synonyms:  MCI-9042

Molecular weight: 466

CAS: 135159-51-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience

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