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 (11):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-160187
    AAA
    		Inhibitor 98.40%
    AAA is a potent blocker of 20-Hydroxyeicosatetraenoic acid (20-HETE) receptor that binds directly to GPR75 and prevents the increases in intracellular Ca2+, IP-1 and β-arrestin.
    AAA
  • HY-12664
    AF64394
    		Inhibitor 98.02%
    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
    AF64394
  • HY-155318A
    GPR3 agonist-2
    		Agonist 99.90%
    GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM.
    GPR3 agonist-2
  • HY-156354
    GPR61 Inverse agonist 1
    		Inhibitor 99.33%
    GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC50: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia.
    GPR61 Inverse agonist 1
  • HY-155417
    GPR34 receptor antagonist 3
    		Antagonist 99.88%
    GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
    GPR34 receptor antagonist 3
  • HY-N15721
    Tryptophan-cholic acid
    		Agonist 98.68%
    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-P991726
    Vemzatatug
    		Inhibitor
    Vemzatatug is a humanized IgG1κ monoclonal antibody inhibitor targeting GPRC5D. Vemzatatug has an antitumor activity. Vemzatatug can be used for cancers like multiple myeloma (MM) research.
    Vemzatatug
  • HY-163087
    PT-91
    		Agonist 98.25%
    PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice.
    PT-91
  • HY-114146
    CID 1375606
    		Agonist 99.90%
    CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
    CID 1375606
  • 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