tgr5

TGR5 is a potent TGR5(GPCR19) agonist.

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.

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

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.

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.

TGR5 agonist 5 (compound K91) is an effective activator of TGR5, with an EC50 of 19 μM in the CRE-Luciferase assay and 30 μM in the cAMP accumulation assay.

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].