1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR4

GPR4

G Protein-Coupled Receptor 4

GPR4 is a proton-sensing G-protein-coupled receptor that is highly expressed in vascular endothelial cells. And GPR4 has emerged as a key regulator of inflammatory responses. GPR4 can be activated by acidosis which is a microenvironment hallmark of numerous pathological conditions such as inflammation, ischemia, and tumors. GPR4 plays a pro-inflammatory role in various pathological conditions. Activation of GPR4 by acidosis stimulates the expression of inflammatory chemokines, cytokines, adhesion molecules and the NF-κB pathway in endothelial cells, increases endothelium-leukocyte adhesion, and facilitates leukocyte infiltration. Moreover, activation of GPR4 by acidosis promotes the endoplasmic reticulum (ER) stress response and apoptosis of endothelial cells. In addition, some studies have demonstrated that GPR4 can promote angiogenesis at acidic pH and is capable of regulating the tube formation, migration, and proliferation of endothelial cells. GPR4 knockout mice displayed altered vessel morphology and reduced vascular length and density.

GPR4 Related Products (2):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101784
    NE 52-QQ57
    99.89%
    NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
    NE 52-QQ57
  • HY-101536
    GPR4 antagonist 1
    Antagonist 98.92%
    GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.
    GPR4 antagonist 1