WNK463 is an orally bioavailable pan-WNK-kinase inhibitor with IC50s of 5, 1, 6, and 9 nM for WNK1, WNK 2, WNK 3, and WNK 4, respectively.
CAS：2012607-27-9
分子式：C21H24F3N7O2
分子量：463.46
纯度：98%
存储：Store at -20°C

Background:

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively[1].

WNK463 (50 nM, 1 μΜ, 10 μΜ; 6 days; Human tissue-engineered corneas (hTECs)) treatment reduces phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

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].

参考文献:
[1]. Yamada K et al. Small-molecule WNK inhibition regulates cardiovascular and renal function. Nat Chem Biol. 2016 Nov;12(11):896-898.
[2]. Desjardins P, et al. Contribution of the WNK1 kinase to corneal wound healing using the tissue-engineered human cornea as an in vitro model. J Tissue Eng Regen Med. 2019 Sep;13(9):1595-1608.