VU0134992 (hydrochloride)

VU0134992 is an inhibitor of inward-rectifier potassium channel 4.1 (K_ir4.1; IC₅₀ = 5.2 µM in a thallium flux assay).¹ It is selective for K_ir4.1 over K_ir2.3, K_ir7.1, and SUR1/K_ir6.2 (IC₅₀s = 13.2, 34.2, and 11.4 µM, respectively), as well as K_ir1.1, K_ir2.1, and K_ir2.2 at 30 µM, but also inhibits K_ir4.2, heteromeric GIRK1/GIRK2, also known as K_ir3.1/K_ir3.2, and heteromeric GIRK1/GIRK4 (IC₅₀s = 8.1, 2.5, and 3.1 µM, respectively). VU0134992 (5 µM) reduces polymyxin B-induced decreases in cell viability in HK-2 human kidney tubular cells and prevents polymyxin B-induced increases in apoptosis in mouse embryonic kidney explant cultures.² In vivo, VU0134992 (50 and 100 mg/kg) increases urine volume and urinary sodium and potassium levels in rats.¹

WARNING This product is not for human or veterinary use.

1. Kharade, S.V., Kurata, H., Bender, A.M., et al. Discovery, characterization, and effects on renal fluid and electrolyte excretion of the K_ir4.1 potassium channel pore blocker, VU0134992. Mol. Pharmacol. 94(2), 926-937 (2018).

2. Lu, J., Azad, M.A.K., Moreau, J.L.M., et al. Inwardly rectifying potassium channels mediate polymyxin-induced nephrotoxicity. Cell. Mol. Life Sci. 79(6), 296 (2022).