TRPV4 Inhibitor

GSK3527497 is an orally active TRPV4 inhibitor. GSK3527497 is applicable for the research of heart failure.

GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC₅₀s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research.

Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus.

SK2220691 is a potent TRPV4 inhibitor. SK2220691 inhibits pulmonary edema induced by GSK1016790. SK2220691 inhibits HCl-induced increases in key factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF).

TRPV4-IN-5 (Compound 1f) is a potent TRPV4 inhibitor (IC₅₀ = 0.46 μM). TRPV4-IN-5 significantly alleviates the symptoms of acute lung injury induced by lipopolysaccharide (HY-D1056) in mice.

TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis.