gpcr19

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 sodium salt (Sodium deoxycholate) can activate the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

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.

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,

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

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

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.

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.

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.

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).

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.

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

TGR5 is a potent TGR5(GPCR19) agonist.

SB756050 is a specific TGR5 agonist.

Ursodeoxycholic acid (UDCA) can be used to dissolve gallstones and reduce cholesterol absorption.

PEN(mouse) acetate (proSAAS(221-242) Acetate) (1236955-25-1 Free base) is a polypeptide derivative.

PEN (rat) is an Endogenous peptide GPR83 agonist. ProSAAS-derived neuropeptide.

Endogenous peptide GPR83 agonist. ProSAAS-derived neuropeptide. Activates phospholipase C (PLC)-mediated signaling cascade in mouse hypothalamus.

PEN (human) is an Endogenous peptide GPR83 agonist. ProSAAS-derived neuropeptide.