RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays).
|1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg. Med. Chem. Lett. 25(18), 4011-4015 (2015).