TGR5 Receptor AgonistTGR5 Receptor Agonist
MedChemExpress (MCE)
HY-14229
1197300-24-5
CCDC
99.71%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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.
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].
TGR5[1] 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6J mice [12-18 weeks
TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)][2]
| | | |
| | | | | |
[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. [Content Brief]
[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. [Content Brief]
[3]. Castellanos-Jankiewicz A, et al. Hypothalamic bile acid-TGR5 signaling protects from obesity. Cell Metab. 2021 Jul 6
33(7):1483-1492.e10. [Content Brief]