g-protein coupled receptor 19

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 (DCA) is a natural product and a TGR5 receptor agonist with cell permeability and oral activity. As a metabolite of intestinal flora, this compound is widely used in research on bile acid signal transduction, glucose and lipid metabolism, and anti-inflammatory mechanisms, and has shown therapeutic potential in diabetes and liver disease models.

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.

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

TGR5 is a potent TGR5(GPCR19) agonist.

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

SB756050 is a specific TGR5 agonist.

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

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.