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Medchemexpress LLC N-(4-((4-isopropylpiperazin-1-yl)sulfonylphenyl)-5-pentafluorophenyl)nicotinamide | 1803003-65-7 | 99.9% | 513.54 | 5 MG
Supplier: Medchemexpress LLC HY1609005MG
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.
- IC50 for human TRPV4 is 0.26 μM.
- IC50 for rat TRPV4 is 0.39 μM.
- Antagonist activity at human TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 minutes.
- Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 minutes.
- Pharmacokinetic analysis has been performed in Wistar rats.
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