For research use only. Not for therapeutic Use.
The TGR5 Receptor Agonist (Cat No.:I000723) is a potent agonist of the TGR5 receptor, also known as GPCR19. This compound has demonstrated improved potency in various cell assays. In U2-OS cells, it exhibited a pEC50 value of 6.8, indicating its ability to activate the TGR5 receptor. Similarly, in melanophore cells, the agonist displayed a pEC50 value of 7.5, suggesting its effectiveness in stimulating TGR5 receptor-mediated responses. The activation of TGR5 by this agonist may have implications in various physiological and pharmacological processes that involve TGR5 signaling.
| Catalog Number | I000723 |
| CAS Number | 1197300-24-5 |
| Synonyms | 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-4-isoxazolecarboxamide |
| Molecular Formula | C18H14Cl2N2O2 |
| Purity | ≥95% |
| Target | TGR5 |
| Solubility | DMSO: ≥ 48 mg/mL |
| Storage | -20°C |
| IC50 | 6.8 (pEC50, U2-OS cell assay); 7.5(pEC50, melanophore cell) |
| IUPAC Name | 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-1,2-oxazole-4-carboxamide |
| InChI | 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 |
| InChIKey | IGRCWJPBLWGNPX-UHFFFAOYSA-N |
| SMILES | CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N(C)C3=CC=C(C=C3)Cl |
| Reference | 1:ACS Med Chem Lett. 2015 Nov 20;7(1):51-5. doi: 10.1021/acsmedchemlett.5b00323. eCollection 2016 Jan 14. Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist.Agarwal S,Patil A,Aware U,Deshmukh P,Darji B,Sasane S,Sairam KV,Priyadarsiny P,Giri P,Patel H,Giri S,Jain M,Desai RC, PMID: 26819665 PMCID: PMC4716599 DOI: 10.1021/acsmedchemlett.5b00323 </br><span>Abstract:</span> TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (hTGR5 EC50 = 57 pM, mTGR5 = 62 pM) with a favorable pharmacokinetic profile. The compound 6g was found to have potent glucose lowering effects in vivo during an oral glucose tolerance test in DIO C57 mice with ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg. |
