Description | HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. |
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Targets | mTRPV4 [1](Cell-free assay) | hTRPV4 [1](Cell-free assay) | rTRPV4 [1](Cell-free assay) | 17 nM | 48 nM | 133 nM |
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In vivo | HC-067047 causes a significant increase in functional bladder capacity in mice and rats suffering from cystitis, thus providing proof of principle that pharmacological inhibition of TRPV4 can be used to treat bladder dysfunction.HC-067047 had no effect on the cystometric parameters of Trpv4−/− mice demonstrates that the observed in vivo effects are specific.[1] |
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