A nonpeptide AT1 receptor antagonist (Ki = 29 nM in rat lung membranes); selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla)

BIBS39 – 5 mg

Brand:
Cayman
CAS:
133085-33-3
Storage:
-20
UN-No:
Non-Hazardous - /

BIBS39 is a nonpeptide antagonist of the angiotensin II type 1 (AT1) receptor (Ki = 29 nM in rat lung membranes).{46447} It is selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla), as well as α1-, α2-, β1-, and β2-adrenergic, adenosine A1 and A2, muscarinic M1, M2, and M3, and atrial natriuretic peptide receptors (Kis = >100 µM for all). BIBS39 (0.3-10 mg/kg) decreases diastolic blood pressure in pithed normotensive rats without affecting heart rate and in renal hypertensive rats with an increase in heart rate when administered at doses ranging from 1 to 30 mg/kg.{46447,46448}  

 

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SKU: 22932 - 5 mg Category:

Description

A nonpeptide AT1 receptor antagonist (Ki = 29 nM in rat lung membranes); selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla), as well as α1-, α2-, β1-, and β2-adrenergic, adenosine A1 and A2, muscarinic M1, M2, and M3, and atrial natriuretic peptide receptors (Kis = >100 µM for all); decreases diastolic blood pressure in pithed normotensive rats without affecting heart rate at 0.3-10 mg/kg; decreases diastolic blood pressure in renal hypertensive rats with an increase in heart rate at 1-30 mg/kg

Formal name: 4′-[[2-butyl-6-[[(cyclohexylamino)carbonyl]amino]-1H-benzimidazol-1-yl]methyl]-[1,1′-biphenyl]-2-carboxylic acid

Synonyms: 

Molecular weight: 524.7

CAS: 133085-33-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Vasodilation

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