| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Pharmacokinetic Analysis in Wistar rats[1]
| Route | Dose (mg/kg) | Cl (L·h/kg) | AUCinf (min·ng/mL) | Vss (L/kg) | T1/2 (h) | | i.v. | 1.05 | 1.35 | 46767 | 2.01 | 1.03 | | Route | Dose (mg/kg) | Cmax (ng/mL) | AUCinf (min·ng/mL) | F (%) | | | p.o. | 1.80 | 143 | 18153 | 22.7 | |
| [IC 50]
hTRPV4: 0.26 μM (IC50); rTRPV4: 0.39 μM (IC50) | [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. DOI:10.1016/j.bmcl.2015.06.098 |
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