2. Signaling Pathways
  3. GPCR/G Protein
  4. Orphan Receptor
  5. Orphan Receptor Antagonist

Orphan Receptor Antagonist

Orphan Receptor Antagonists (6):

Cat. No. Product Name Effect Purity
  • HY-108469
    BI-6015
    		Antagonist 99.44%
    BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.
  • HY-101483
    Dihydromunduletone
    		Antagonist 99.96%
    Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
  • 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 .
  • HY-135589
    7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene
    		Antagonist 99.77%
    7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is a liver receptor homolog-1 (LRH-1) antagonist with an IC50 of 3.1 μM.
  • HY-148259
    SF-1 antagonist-1
    		Antagonist
    SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer.
  • HY-159920
    PSB-22269
    		Antagonist
    PSB-22269 is a GPR17 antagonist with a Ki value of 8.91 nM. PSB-22269 further demonstrated significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies revealed that the binding site of PSB-22269 contains positively charged arginine residues and a hydrophobic pocket. PSB-22269 provides a strategy to promote remyelination and holds promise for research in the field of multiple sclerosis.