trpv4

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).

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

RN9893 is a selective and potent TRPV4 receptor antagonist with IC50 values of 320, 420 and 660 nM for TRPV4 receptors in mouse, human and rat, respectively.

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

RN-1665 is a potent and selective TRPV4 receptor antagonist.

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

TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).

TRPV4 antagonist 4, a potent inhibitor of TRPV4 with an IC50 of 22.65 nM, effectively blocks TRPV4 current and demonstrates protective properties against acute lung injury [1].

TRPV4-IN-5 (Compound 1f) is an effective TRPV4 inhibitor with an IC50 value of 0.46 μM. It significantly alleviates symptoms of acute lung injury in mice induced by lipopolysaccharide.

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).

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.

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

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

RQ-00203078 is a highly selective, potent, and orally available TRPM8 antagonist.

4alpha-PDD activates transient receptor potential vanilloid 4 (TRPV4) channels and is inactive for signaling through PKC.

N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretion from 832/13 INS-1 pancreatic β-cells. The levels of N-arachidonoyl taurine are changed in mouse brain following administration of δ9-tetrahydrocannabinol (δ9-THC).

SET 2 is an antagonist of transient receptor potential vanilloid type 2(TRPV2) with an IC50 of 0.46 μM. SET 2 shows selectivity over TRPV1, TRPV3 and TRPV4.

RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). |1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg. Med. Chem. Lett. 25(18), 4011-4015 (2015).

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

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist, effectively and reversibly inhibiting currents through human, rat, and mouse TRPV4 orthologs with IC50 values of 486 nM, 133 nM, and 17 nM, respectively.

JNc-440 is a potent anti-hypertensive agent. jNc-440 enhances the interaction between the transient receptor potential vanilloid subtype 4 (TRPV4) and calcium-activated potassium channel 3 (KCa2.3) in endothelial cells. jNc-440 also increases vasodilation and has hypotensive activity in mice.

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.

GSK3527497 is a potent and selective inhibitor of Transient Receptor Potential Vanilloid‑4 (TRPV4) with IC50 = 12 nM) for the treatment of heart failure and respiratory diseases. GSK3527497 is a preclinical candidate suitable for oral and iv administration that is projected to inhibit TRPV4 effectively in patients from a low daily clinical dose.

GSK3527497 is a novel potent and selective inhibitor of transient receptor potential vanilloid-4 (TRPV4).