2. Signaling Pathways
  3. GPCR/G Protein
  4. Orphan GPCR

Orphan GPCR

Rrphan G protein-coupled receptor

Orphan GPCRs (orphan G protein-coupled receptors) are receptors lacking endogenous ligands. GPCRs are th largest family of transmembrane receptors and have over the past decades developed into highly successful drug targets. However, many GPCRs are still orphans and the function is enigmatic. Orphan GPCRs account for ∼30% of the ∼400 non-olfactory human GPCRs. In terms of orphan GPCR ligands, initial efforts focused on identifying novel neuropeptides since orphan GPCR expression was located primarily in the brain. G protein coupling of unliganded orphan GPCRs—GPR22, GPR137b, GPR88, GPR156, GPR158, GPR179, GPRC5D and GPRC6A—with pathophysiological association were accurately detected using luciferase reporter assays[1][2].

Orphan GPCR Related Products (3):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N15721
    Tryptophan-cholic acid
    		Agonist
    Tryptophan-cholic acid (Trp-CA) is a microbial amino-acid-conjugated bile acid, serving as an endogenous ligand and agonist of the orphan G protein-coupled receptor (GPCR) MRGPRE. Tryptophan-cholic acid activates MRGPRE, promoting the secretion of glucagon-like peptide-1 (GLP-1) through the Gs-cAMP and β-arrestin-1-ALDOA signaling pathways, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid is promising for research of type 2 diabetes.
    Tryptophan-cholic acid
  • HY-P991587
    SAR-446523
    		Inhibitor
    SAR-446523 is a humanized IgG1 monoclonal antibody inhibitor targeting GPRC5D. SAR-446523 significantly induces antibody-dependent cell-mediated cytotoxicity (ADCC). SAR-446523 has potent antitumor activity with improvement of mouse survival in NK humanized NOG huIL15 transgenic mice model bearing MM cells. SAR-446523 can be used for multiple myeloma (MM) research.
    SAR-446523
  • HY-160187A
    (Rac)-AAA
    		Inducer
    (Rac)-AAA is the racemate of AAA. (Rac)-AAA is an antagonist of 20-HETE receptor. (Rac)-AAA can increase the expression of GPR75 receptor in androgen-insensitive prostate cancer cells. (Rac)-AAA dose-dependently increases p38 phosphorylation. (Rac)-AAA induces a significant decrease in the phosphor-AKT signal in nuclei of cells. (Rac)-AAA mitigates the NF-κB signal in unstimulated cell nuclei. (Rac)-AAA can diminish the membrane associated signal intensity. (Rac)-AAA decreases the FAK phosphorylation induced by 20-HETE.
    (Rac)-AAA