Background:

TGR5 Receptor Agonist is a potent and selective agonist of TGR5 G-protein receptor with a pEC50 value of 6.8 in the U2-OS cell assay [1].

TGR5 Receptor Agonist has been shown the activated potency of TGR5 receptor with pEC50 values of 6.8 and 7.5 in the U2-OS cells and melanophire cells assay, respectively. In addition, TGR5 Receptor Agonist has been found to be fully specific for the human TGR5 receptor in the U2-OS and melanophore cell lines and also selective against other 7TM receptors. Besides, TGR5 Receptor Agonist has been reported to have physicochemical properties and no measurable activity against the common cytochrome P450 (CYP450) isoforms or hERG dofetilide binding with a pIC50 value of<4.3.

参考文献:
[1] Evans KA1, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem. 2009 Dec 24;52(24):7962-5.