gsk-2798745

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.

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.

(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.