tgr 5

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.

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) is a potent inhibitor of liver-specific fatty acid transporter 5 (FATP5). Ursodeoxycholic acid inhibits cholesterol absorption and is used to dissolve gallstones.

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.

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.

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

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

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.

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