RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 µM, an IC50 >30 µM against TRPV3, an IC50 of approximately 30 µM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
General description
RN-9893 is a small, orally bioavailable antagonist of TRPV4 (transient receptor potential subfamily V4. It is a tri-substituted benzamide compound.