TGR5 Receptor Agonist

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). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM). 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. It also inhibits the cytochrome P450 (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. CAS Number: 1197300-24-5. Molecular Formula: C18H14Cl2N2O2. Formula Weight: 361.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 50 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 30 mg/ml. SMILES: ClC1=C(C2=NOC(C)=C2C(N(C3=CC=C(Cl)C=C3)C)=O)C=CC=C1. InChi Code: InChI=1S/C18H14Cl2N2O2/c1-11-16(17(21-24-11)14-5-3-4-6-15(14)20)18(23)22(2)13-9-7-12(19)8-10-13/h3-10H,1-2H3. InChi Key: IGRCWJPBLWGNPX-UHFFFAOYSA-N.