1669444-50-1

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

PF-05214030 is a TRPV4 antagonist (IC50: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist[1][2].

[1] Jiang Y, et al. Targeting extracellular matrix stiffness and mechanotransducers to improve cancer therapy. J Hematol Oncol. 2022 Mar 24;15(1):34. DOI:10.1186/s13045-022-01252-0
[2] Sarah Skerratt, et al. The Discovery and Optimisation of a Highly Selective Series of TRPV4 Antagonists.