A GCGR antagonist (Ki = 14 nM for the human recombinant receptor); greater than 230-fold selective for GCGR over the GLP-1 receptor

Glucagon Receptor Antagonist 4 – 25 mg

Brand:
Cayman
CAS:
1393124-08-7
Storage:
-20
UN-No:
Non-Hazardous - /

Glucagon receptor antagonist 4 is an antagonist of the glucagon receptor (GCGR; Ki = 14 nM for the human recombinant receptor).{42993} It is greater than 230-fold selective for GCGR over the glucagon-like peptide 1 (GLP-1) receptor, as well as a panel of 69 receptors, ion channels, uptake sites, and enzymes at 10 µM. Glucagon receptor antagonist 4 prevents glucagon-induced increases in glucose levels in rat blood when administered at doses of 7.5 and 75 mg/kg.  

 

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Description

A GCGR antagonist (Ki = 14 nM for the human recombinant receptor); greater than 230-fold selective for GCGR over the GLP-1 receptor, as well as a panel of 69 receptors, ion channels, uptake sites, and enzymes at 10 µM; prevents glucagon-induced increases in glucose levels in rat blood at 7.5 and 75 mg/kg,,

Formal name: N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-β-alanine

Synonyms:  GCGR Antagonist IV

Molecular weight: 503.5

CAS: 1393124-08-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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