N-[4-[[4-(1-Methylethyl)-1-piperazinyl]sulfonyl]phenyl]-2-nitro-4-(trifluoromethyl)benzamide hydrochloride

Uses

RN 9893 Hydrochloride is a selective TRPV4 inhibitor.

Biological Activity

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, r at 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.