2215852-91-6

GSK3395879 is a potent, selective and orally active TRPV4 inhibitor (IC50 = 1 nM), GSK3395879 demonstrated the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model. GSK3395879 is a tool for studying the biology of TRPV4 and an advanced lead for identifying new heart failure medicines.

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

[1] Brnardic EJ, et al. Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem. 2018 Nov 8;61(21):9738-9755. DOI:10.1021/acs.jmedchem.8b01317