2. Signaling Pathways
  3. GPCR/G Protein
  4. G protein-coupled Bile Acid Receptor 1
  5. G protein-coupled Bile Acid Receptor 1 Agonist

G protein-coupled Bile Acid Receptor 1 Agonist

G protein-coupled Bile Acid Receptor 1 Agonists (24):

Cat. No. Product Name Effect Purity
  • HY-15677
    INT-777
    		Agonist ≥98.0%
    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
  • HY-N0169
    Hyodeoxycholic acid
    		Agonist 99.87%
    Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
  • HY-155307
    TGR5 agonist 4
    		Agonist
    TGR5 agonist 4 (compound 19), a cholic acid derivative, is a selective TGR5 agonist with an EC50 of 4 μM.
  • HY-116453
    RO5527239
    		Agonist
    RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2.
  • HY-14229
    TGR5 Receptor Agonist
    		Agonist 99.86%
    TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.
  • HY-12434
    INT-767
    		Agonist ≥98.0%
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
  • HY-110173
    TC-G 1005
    		Agonist 99.83%
    TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
  • HY-102016
    SB756050
    		Agonist 98.49%
    SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
  • HY-P2278
    PEN (human)
    		Agonist 99.68%
    PEN (human), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
  • HY-101274
    BAR501
    		Agonist ≥98.0%
    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
  • HY-15677A
    INT-777 (R-enantiomer)
    		Agonist 98.73%
    INT-777 (R-enantiomer) is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.
  • HY-101273
    BAR502
    		Agonist 99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  • HY-145234
    GPBAR1-IN-3
    		Agonist
    GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.
  • HY-P2277A
    PEN (rat) (TFA)
    		Agonist
    PEN (rat) TFA, one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
  • HY-107612
    GPBAR-A
    		Agonist
    GPBAR-A is a specific agonist of the bile acid receptor GPBAR1. GPBAR-A can be used for the research of diabetes mellitus.
  • HY-149807
    TGR5 agonist 1
    		Agonist
    TGR5 agonist 1 (compound 18) is a potent TGR5 agonist with an EC50 value of 0.31 µM.
  • HY-P2277
    PEN (rat)
    		Agonist
    PEN (rat), one of the most abundant hypothalamic neuropeptide and derived from the proprotein ProSAAS, is an endogenous ligand of GPR83.
  • HY-142159
    FXR/TGR5 agonist 1
    		Agonist
    FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.
  • HY-147086
    CAY10789
    		Agonist
    CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
  • HY-146453
    TGR5 Receptor Agonist 3
    		Agonist
    TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.