TGR5 Receptor Agonist

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].

Product Specifications

CAS Number

[1197300-24-5]

Product Name Alternative

CCDC

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

Calcium Channel; G protein-coupled Bile Acid Receptor 1

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/TGR5-Receptor-Agonist.html

Purity

99.71

Solubility

DMSO : ≥ 48 mg/mL

Smiles

ClC1=CC=CC=C1C2=NOC(C)=C2C(N(C)C3=CC=C(Cl)C=C3)=O

Molecular Formula

C18H14Cl2N2O2

Molecular Weight

361.22

Precautions

H302, H315, H320, H335

References & Citations

[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.