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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[1].

hTRPV4: 0.26 μM (IC₅₀); rTRPV4: 0.39 μM (IC₅₀)

[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. DOI:10.1016/j.bmcl.2015.06.098