NE 52-QQ57 (GPR4 antagonist 13) is a potent, elective, and efficacious GPR4 antagonist with IC50 of 70 nM (hGPR4).
GPR4 antagonist 13 displays no significant inhibition against a panel of enzymes, receptors, and ion channels.
GPR4 antagonist 13 is also selective over the related proton sensing receptors OGR1 and TDAG8.
GPR4 antagonist 13 weakly inhibits rat GPR4 with IC50 of 1.84 uM.
GPR4 antagonist 13 shows significant efficacy in the rat antigen induced arthritis as well as in the hyperalgesia and angiogenesis model at a well-tolerated dose of 30 mg/kg.
