WNK463

2012607-27-9

463.46

DMSO : >= 30 mg/mL (64.73 mM)

Metabolic Enzyme/Protease

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC_50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively^[1]. IC50 & Target: IC50: 5 nM (WNK1), 1 nM (WNK2), 6 nM (WNK3), and 9 nM (WNK4)^[1] In Vitro: WNK463 (50 nM, 1 umy, 10 umy; 6 days; Human tissue-engineered corneas (hTECs)) treatment reduces phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs. In Vivo: WNK463 (1-10 mg/kg; oral administration; 4 hours; Spontaneously hypertensive Sprague Dawley rats) treatment produces dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. WNK463 produces significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates.
WNK463 is orally bioavailable in Sprague Dawley rats with a half-life of 2.1 hours^[1].