1. GPCR/G Protein
  2. GPCR19

GPCR19

GPCR19 (G-protein coupled receptor 19, GPBAR1) is a protein that in humans is encoded by the GPBAR1 gene. This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. GPCR19 functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids. One effect of this receptor is to activate deiodinases which convert the prohormone thyroxine (T4) to the active hormone triiodothyronine (T3). T3 in turn activates the thyroid hormone receptor which increases metabolic rate.

GPCR19 Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-15677
    INT-777 Agonist >98.0%
    INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM.
  • HY-12434
    INT-767 Agonist >98.0%
    INT-767 is a potent agonist for both FXR (mean EC50, 30 nM by PerkinElmer AlphaScreen assay) and TGR5 (mean EC50, 630 nM by time resolved-fluorescence resonance energy transfer).
  • HY-14229
    TGR5 Receptor Agonist Agonist 99.86%
    TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).
  • HY-101274
    BAR501 Agonist 98.82%
    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
  • HY-15677A
    INT-777 R-enantiomer Agonist
    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-N0593A
    Deoxycholic acid sodium salt Activator
    Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-102016
    SB756050 Agonist 99.02%
    SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
  • HY-101273
    BAR502 Agonist >98.0%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  • HY-N0593
    Deoxycholic acid Activator >98.0%
    Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.