htrpv4

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

HC-067047 is a potent and selective TRPV4 antagonist that also inhibits the endogenous TRPV4-mediated response to 4α-PDH.

RN-1734 is selective TRPV4 channel antagonist(IC50 of 2.3 μM,5.9 μM,3.2 μM for hTRPV4, mTRPV4 and rTRPV4,respectively)

TRPV4 agonist-1 free base (OUN67600) is an agonist of transient receptor potential vanilloid 4 (TRPV4;EC50 of 60 nM, in the hTRPV4 Ca2+ assay).

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonist (EC50: hTRPV4 of 0.77 μM, mTRPV4 of 4.0 μM, and rTRPV4 of 4.1 μM) and also acts as an antagonist for TRPM8 (IC50: 4 μM).

GSK3395879 is a selective, orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) with an IC50 of 1 nM for hTRPV4.

GSK2798745 is an orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker (IC50s: 1.8 and 1.6 nM for hTRPV4 and rTRPV4). It is used in research for the treatment of pulmonary edema associated with congestive heart failure.

PF-05214030 is a novel potent TRPV4 antagonist (hTRPV4 IC50 4nM; rTRPV4 IC50 27nM).

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

TRPV4 agonist-1 is an agonist of TRPV4 (EC50: 60 nM in the hTRPV4 Ca2+ assay).