GPR4 antagonist 3b

The first potent and selective proton-sensing GPCR GPR4 antagonist with IC50 of 67 nM, with no activity against TDAG8 and OGR1 (IC50>10 uM); effectively prolongs life in the mouse myocardial infarction model in vivo, and is a very effective tool for investigating the physiologic and pharmacologic roles of GPR4.

References 1. Fukuda H, et al. ACS Med Chem Lett. 2016 Feb 24;7(5):493-7. 2. Tobo A, et al. PLoS One. 2015 Jun 12;10(6):e0129334. View Related Products by Target Proton-sensing GPCRs