| References: |
HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). target: TRPV4 IC 50: 48 ± 6 nM (human), 133 ± 25 nM (rat) , and 17 ± 3 nM (mouse) 1) The reference for administration of HC-067047 is 10 mg/kg (i.P) 2) HC-067047 caused a significant reduction of the maximal micturition pressure in rats, which might be caused by an effect on TRPV4 in smooth muscle. 3) HC-067047 Reduces Pollakisuria and Increases Functional Bladder Capacity 4) HC-067047 exhibits high selectivity toward TRPV4: IC50 values were at least 100-fold higher for the closely related channels TRPV1, TRPV2, and TRPV3, and 10-fold higher for TRPM8 and hERG. |
