TGR5 Receptor Agonist_product_DataBase

Bioactivity

TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity[1][2][3][4].

Target

TGR5

In Vivo

TGR5 Receptor Agonist (CCDC) activates directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons and a small percentage of non-neuronal cells in Trpv1-/- mice[2].TGR5 Receptor Agonist (CCDC) (2 or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice[3]. Animal Model:

Name

TGR5 Receptor Agonist

CAS

1197300-24-5

Formula

C18H14Cl2N2O2

Molar Mass

361.22

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Evans KA, et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem. 2009 Dec 24;52(24):7962-5. [2]. Caldwell A, Grundy L, Harrington AM, Garcia-Caraballo S, Castro J, Bunnett NW, Brierley SM. TGR5 agonists induce peripheral and central hypersensitivity to bladder distension. Sci Rep. 2022 Jun 15;12(1):9920. [3]. Castellanos-Jankiewicz A, et al. Hypothalamic bile acid-TGR5 signaling protects from obesity. Cell Metab. 2021 Jul 6;33(7):1483-1492.e10.

PeptideDB

TGR5 Receptor Agonist

CAS: 1197300-24-5 F: C18H14Cl2N2O2 W: 361.22