A potent and selective AT1 receptor antagonist (IC50s = 7.7 and >100

Olmesartan – 250 mg

Brand:
Cayman
CAS:
144689-24-7
Storage:
-20
UN-No:
Non-Hazardous - /

Olmesartan is a potent and selective non-peptide angiotensin II receptor 1 (AT1) antagonist (IC50s = 7.7 and >100,000 nM for AT1 and AT2, respectively, in a radioligand binding assay).{20965} It reduces contraction of isolated guinea pig aorta induced by angiotensin II (Item No. 17150; pD2 = 9.9) but not phenylephrine (Item Nos. 17205 | 18619) or potassium chloride. Olmesartan (0.01 and 0.03 mg/kg, i.v.) reduces the angiotensin II-induced pressor response in conscious normotensive rats with the maximum effect occurring one hour after administration and decreasing thereafter. The oral prodrug form of olmesartan, olmesartan medoxomil (Item No. 11614), has an increased duration of action with no decrease in efficacy eight hours post administration in normotensive rats.  

 

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Description

A potent and selective AT1 receptor antagonist (IC50s = 7.7 and >100,000 nM for AT1 and AT2, respectively, in a radioligand binding assay); reduces angiotensin II-induced contractions of isolated guinea pig aorta (pD2 = 9.9); reduces the angiotensin II-induced pressor response in conscious normotensive rats

Formal name: 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid

Synonyms:  CS 088|RNH 6270

Molecular weight: 446.5

CAS: 144689-24-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation

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