gpcr19

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.

PEN (human) aceate, one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.

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.

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.

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

Sodium taurodeoxycholate hydrate (Taurodeoxycholic acid sodium salt monohydrate) has been used in a study to assess the effect of submicellar concentrations of bile salts on the lipid bilayer membrane.

Taurodeoxycholate sodium salt (Sodium taurodeoxylate) is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. and it inhibits various inflammatory responses

Hyodeoxycholic acid-D5 is the deuterated form of Hyodeoxycholic acid (TMSM-3213). This compound is a secondary bile acid formed by gut microbiota in the small intestine and acts as an agonist for TGR5 (GPCR19), with an EC50 value of 31.6 µM in CHO cells.

Ursodeoxycholic acid-D5 is the deuterated form of Ursodeoxycholic acid. Ursodeoxycholic acid (T0700) (Ursodeoxycholate) is a secondary bile acid produced through the transformation of (cheno)deoxycholic acid by intestinal bacteria. It plays a crucial role in maintaining intestinal barrier integrity and is essential for lipid metabolism. As a signaling molecule, Ursodeoxycholic acid (T0700) functions by interacting with bile acid-activated receptors, including the G protein-coupled bile acid receptor 5 (TGR5, GPCR19) and the Farnesoid X receptor (FXR). It is used in research related to various liver and gastrointestinal disorders and is effective when administered orally.

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

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.

RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly more potent than Betulinic acid (EC50= 1.04 μM). It exhibits much higher selectivity for TGR5 over FXRα. The compound enhances mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. Additionally, RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 cells and microglia. RG-239 is applicable for research related to type 2 diabetes.

GPBAR-A is a synthetic small-molecule agonist of GPBAR1, also known as TGR5, that activates this G protein–coupled bile acid receptor involved in energy homeostasis, glucose metabolism, and immune regulation, GPBAR-A is extensively studied for its therapeutic potential in metabolic disorders such as type 2 diabetes, obesity, and inflammation-related diseases.