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.

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.

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

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

TRPV4 antagonist 5 is a TRPV4 inhibitor described in WO2025014818 and a derivative of GSK2798745 (T15434), with potential applications in research on pain, lung injury, inflammation, and skeletal developmental disorders.

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

(Iso)-TRPV4 antagonist 5 are potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) channel blockers for the treatment of pulmonary edema and respiratory diseases. This compound was discovered through optimization of a spirocarbamate lead designed to reduce interstitial lung fluid. Research on its derivatives and related compounds primarily focuses on improving metabolic stability, reducing lipophilicity to enhance clearance, and increasing potency.

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-KCa2.3 modulator 1 (Compound IB-2) is a TRPV4-KCa2.3 protein complex activator with antihypertensive properties. It enhances endothelial cell hyperpolarization and vasodilation, making it a promising candidate for research in hypertension and cardiovascular diseases.

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.

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

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).

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

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.

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

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.

SK2220691 is a potent TRPV4 inhibitor. It effectively suppresses pulmonary edema induced by GSK1016790. Additionally, SK2220691 inhibits the increase of crucial factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF) induced by hydrochloric acid.

TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 value of 8.1. It displays excellent selectivity for related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4) with selectivity greater than 100-fold. TRPM5 agonist-1 induces local stimulation of gastrointestinal transit in mice and is useful for studying the promotion of gastric motility.