An agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays); stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM); increases GLP-1 secretion and decreases glucose levels in the hepatic portal vein in dogs at 1 mg/kg when administered in combination with glucose; inhibits the CYP isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1

TGR5 Receptor Agonist – 1 mg

Brand:
Cayman
CAS:
1197300-24-5
Storage:
-20
UN-No:
Non-Hazardous - /

TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).{27533} It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).{27534} TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.{27533} It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).  

 

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Description

An agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays); stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM); increases GLP-1 secretion and decreases glucose levels in the hepatic portal vein in dogs at 1 mg/kg when administered in combination with glucose; inhibits the CYP isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively)

Formal name: 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-4-isoxazolecarboxamide

Synonyms: 

Molecular weight: 361.2

CAS: 1197300-24-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Research Area|Endocrinology & Metabolism|Bile Acids & Microbiome||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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