RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively.
Pharmacokinetic Analysis in Wistar rats[1]
References:
[1]. Wei ZL, et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5.