TGR5 Receptor Agonist

• UNSPSC Description:

  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 Antigen:

  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

• Solubility:

  DMSO : ≥ 48 mg/mL

• Smiles:

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

• Molecular Weight:

  361.22

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  1197300-24-5