TGR5 Receptor Agonist

Biological Activity

TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).TGR5 Receptor Agonist has good physicochemical properties.But it has no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50 <4.3).GR5 receptor agonists are potentially useful therapeutics for metabolic disorders like type II diabetes and its associated complications.

Customer Product Validations & Biological Datas

	Source	Sci Rep (2018). Figure 5. TGR5
	Method	TGR5KO cells
	Cell Lines	NRVMs
	Concentrations	10–100 μM
	Incubation Time	10–15 mins
	Results	NMVMs in culture show spontaneous contraction. Incubation with INT-777, in the range of 10–100 μM, does not change the contraction rate of NMVMs in both wild type and TGR5KO cells

Chemical Information

Molecular Weight	361.22
Formula	C18H14Cl2N2O2
CAS Number	1197300-24-5
Solubility (25°C)	DMSO ≥ 30 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Evans KA,et al. J Med Chem. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.