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, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.

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).

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.

TGR5 agonist 8 (Compound 7i) is a TGR5 activator with an EC₅₀ of 571 nM. It significantly reduces blood glucose levels and food intake in mice with acute diabetes and suppresses appetite over a longer period. TGR5 agonist 8 is applicable for research in diabetes and obesity.

TGR5 agonist 9 is a highly selective, orally active allosteric agonist of TGR5, exhibiting EC₅₀ values of 0.48 μM for hTGR5 and 0.49 μM for mTGR5. It recruits β-arrestin 1 (EC₅₀= 78.8 μM) and β-arrestin 2 (EC₅₀= 12.3 μM), and demonstrates enhanced efficacy in cAMP accumulation (EC₅₀= 0.48 μM). In ICR mouse models, TGR5 agonist 9 shows significant hypoglycemic effects, making it a potential candidate 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].