A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (Ki = 3.7 nM); a partial agonist of PPARγ

Telmisartan – 500 mg

Brand:
Cayman
CAS:
144701-48-4
Storage:
-20
UN-No:
Non-Hazardous - /

Angiotensin II is a peptide hormone which regulates blood pressure and fluid balance, contributing to hypertension, atherosclerosis, left ventricular hypertrophy, myocardial infarction, and heart failure.{20935} Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (Ki = 3.7 nM).{20934} It also acts as a partial agonist of PPARγ, activating the receptor to 25-30% of that produced by the full agonist rosiglitazone (EC50 = 4.5 μM).{20930} Through these actions, telmisartan potently reduces blood pressure in various animal models of hypertension, diminishing cardiac hypertrophy, cardiovascular and renal risk, and glomerulosclerosis.{20932,20931,20933}  

 

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Description

A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (Ki = 3.7 nM); a partial agonist of PPARγ, activating the receptor to 25-30% of that produced by the full agonist rosiglitazone (EC50 = 4.5 μM); potently reduces blood pressure

Formal name: 4′-[(1,4′-dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl]-[1,1′-biphenyl]-2-carboxylic acid

Synonyms:  BIBR 277|Micardis|Pritor

Molecular weight: 514.6

CAS: 144701-48-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Cardiovascular System|Kidney & Renal Disease

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