GPCR19

Taurodeoxycholic acid (Taurodeoxychloic acid) is a bile acid taurine conjugate of deoxycholic acid, a human metabolite that stabilizes mitochondrial membranes and reduces the formation of free radicals.Taurodeoxycholic acid inhibits apoptosis by blocking calcium-mediated apoptotic pathways and by activation of caspase-12. Taurodeoxycholic acid has neuroprotective activity and has been used to study 3-nitropropionic acid-induced or stabilized hereditary Huntington's chorea (HD).

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.

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.

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

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.

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.

BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1). BAR501 impurity (10 μM) induces a 150% increase in luciferase activity in a GP-BAR1 reporter gene assay

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

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.

Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a hydrophilic bile salt, influences bile salt and biliary lipid secretion in rats.

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.

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

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

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.

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.

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.

SB756050 is a specific TGR5 agonist.

TGR5 is a potent TGR5(GPCR19) agonist.

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

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT7R receptor, with a dissociation constant (K_i) of 6.5 nM.

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].