tgr5

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3 cAMP PKA signaling pathway after subarachnoid hemorrhage in rats.

Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,

Ursodeoxycholic acid (UDCA) can be used to dissolve gallstones and reduce cholesterol absorption.

Deoxycholic acid (Cholanoic Acid) is a bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.

Deoxycholic acid sodium salt (Sodium deoxycholate) can activate the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

Hyodeoxycholic acid (NSC 60672) has been used in trials studying the treatment of Hypercholesterolemia.

SBI-115 is an antagonist of TGR5. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5

TGR5 is a potent TGR5(GPCR19) agonist.

Compound 22b, also known as TGR5 agonist 6, is a non-systemic, intestine-targeted TGR5 agonist that demonstrates significant and sustained blood glucose-lowering effects with an acceptable safety profile.

TGR5 agonist 7 (Compound 22-Na) is an intestine-restricted, orally active agonist of the G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 of less than 1 μM. In mouse models, it demonstrates blood glucose-lowering effects, making it useful for diabetes research.

FXR/TGR5 agonist 1 acts as an agonist on both FXR and TGR5 receptors and is utilized for treating fatty liver disease.

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

Compound 18 (TGR5 agonist 1) is a potent agonist of TGR5, exhibiting an EC50 value of 0.31 µM [1].

TGR5 agonist 2 (compound 19) serves as a highly potent TGR5 agonist, with an EC50 value of 0.27 µM [1].

Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].

TGR5 agonist 4 (compound 19), a cholic acid derivative, selectively activates the TGR5 receptor with an EC50 of 4 μM [1].

TGR5 Receptor Agonist 4, a selective agonist for the Bile Acid Receptor (TGR5), exhibits potent activity with an EC50 of 2 nM for human TGR5 (hTGR5) and 3 nM for mouse TGR5 (mTGR5). It is notably involved in mediating hypoglycemic and weight loss effects [1].

INT-767 is a potent farnesoid X receptor (FXR) TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner.

BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).

INT-777 is the R-enantiomer of INT-777, less potent than INT-777,EC50 of 4.79 μM for TGR5.

TRC210258 is a TGR5 agonist that acts by decreasing glycemic and dyslipidemic cardiovascular risk in animal models of diabesity.

WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-

BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM).