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WNK463

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Chemical Structure| 2012607-27-9 同义名 : -
CAS号 : 2012607-27-9
货号 : A361136
分子式 : C21H24F3N7O2
纯度 : 98%
分子量 : 463.456
MDL号 : MFCD30489744
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

生物活性
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]
实验方案
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
参考文献

[1]Yamada K, Park HM, Rigel DF, et al. Small-molecule WNK inhibition regulates cardiovascular and renal function. Nat Chem Biol. 2016 Nov;12(11):896-898.