WNK463 |
| カタログ番号GC19383 |
WNK463 は、WNK1、WNK2、WNK3、および WNK4 に対してそれぞれ 5 nM、1 nM、6 nM、および 9 nM の IC50 を有する、経口的に生物学的に利用可能なパン-ウィズ-ノ-リジン (K) (WNK)-キナーゼ阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2012607-27-9
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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.
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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