WNK463 is a potant With-No-Lysine (WNK) kinase inhibitor with IC50s of 5/1/6/9 nM for WNK1/2/3/4.
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描述 | The With-No-Lysine (K) (WNK) kinases play an essential role in regulating blood pressure and homeostasis of body fluid and electrolyte. WNK463 is an orally bioavailable pan-WNK-kinase inhibitor that inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4) with IC50 values of 5nM, 1nM, 6nM, and 9nM, respectively. It also inhibits WNK1-catalyzed phosphorylation of the native WNK substrate, oxidative stress response 1, with an IC50 value of 41nM. In spontaneously hypertensive rats (34 – 42 weeks of age), oral administration of WNK463 at doses of 1, 3, or 10mg/kg body weight resulted in a dose-dependent decrease in blood pressure, a simultaneous increase in heart rate, and significant increases in urine output, urinary sodium, and potassium excretion rate[1] |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.16mL 0.43mL 0.22mL |
10.79mL 2.16mL 1.08mL |
21.58mL 4.32mL 2.16mL |
CAS号 | 2012607-27-9 |
分子式 | C21H24F3N7O2 |
分子量 | 463.456 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(64.73 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
5% DMSO+30%PEG 300+5% Tween 80+water 8 mg/mL |