GPCR19

TGR5 is a potent TGR5(GPCR19) agonist.

BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5).

SB756050 is a specific TGR5 agonist.

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

Cholic acid 7-sulfate: a cholic acid metabolite with added sulfate at position 7, increased in feces of male mice with specific diets.

CAY10789: potent CysLT1R antagonist (IC50 2.8 µM), GPBAR1 agonist (EC50 3 µM), reduces U937 cell adhesion, TNF-α, stable with promising pharmacokinetics.

WB403 activates TGR5, lowers fasting/postprandial glucose and HbA1c, enhances glucose tolerance, and normalizes pancreatic α/β-cells in diabetic mice.

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

RO5527239 is a potent, orally available GPBAR1 agonist agent.

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

Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM.

TGR5 agonist 10 is a selective, allosteric, and orally bioavailable agonist for the Takeda G protein-coupled receptor 5 (TGR5), with EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. It demonstrates specificity for TGR5 over FXR and can activate both human and mouse TGR5 to induce cAMP accumulation. The compound enhances cholic acid's functional activity and efficacy on hTGR5 and shows higher selectivity in cAMP formation compared to β-arrestin 2 recruitment. TGR5 agonist 10 exhibits hypoglycemic effects in an oral glucose tolerance test in Mus musculus and can be utilized in diabetes research.

5-HT7R antagonist 1 is a G protein-biased antagonist with Ki of 6.5 nM for 5-HT 7R.

TGR5 Receptor Agonist 3 is a GPBAR1 agonist with EC50 of 16.4 nM (hTGR5) & 209 nM (mTGR5), ensures gallbladder safety and reduces filling.

GPBAR1-IN-3 (Compound 14) is both a selective agonist for GPBAR1, with an EC50 value of 0.17 μM, and an antagonist for CysLT1R [1].

LT-188A is a potent TGR5 agonist with an EC50 value of 23 μM. It effectively reduces levels of inflammatory mediators in macrophages.

5β-Cholestane-3α,7α,12α,25-tetrol is a type of bile acid alcohol that activates the G protein-coupled bile acid receptor 1 (GPBAR1), also known as TGR5, in HEK293 cells that express the human receptor, at concentrations between 0.1 to 10 µM. In individuals with cerebrotendinous xanthomatosis (CTX), a progressive metabolic leukodystrophy, levels of this compound are elevated in the blood, feces, and bile.