货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S58537-1ml促销	10mM in DMSO	￥720.00 ￥648.00 S58537-1ml ￥648.00 现货	4 4	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S58537-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

丝氨酸/苏氨酸激酶抑制剂;Serine/threonin kinase Inhibitors;;InformationWNK463 WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4).TargetsWNK-kinaseIn vitroWNK463 potently inhibited the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). WNK463 also inhibited WNK1-catalyzed phosphorylation of the native WNK substrate, oxidative stress response 1 (OSR1) in a biochemical assay and in human embryonic kidney 293 (HEK293) cells that express exogenous OSR1 and that are activated by sorbitol-mediated osmotic stress.In vivoIn rodent models of hypertension, WNK463 affects blood pressure and body fluid and electrolyte homeostasis. WNK463 is orally bioavailable in C57BL/6 mice (100%) and Sprague Dawley rats (74%), with a half-life of 3.6 and 2.1 h, respectively. In spontaneously hypertensive rats (SHRs), WNK463 administered orally (p.o.) at 1, 3, or 10 mg per kg body weight (mg/kg) p.o. achieved maximum plasma concentration (Cmax) values of 88, 441, and 1,170 nM, respectively. These exposures produced dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. Moreover, WNK463 produced significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates. Orally administered WNK463 also significantly decreasedblood pressure in these hypertensive mice. WNK463 elicited in vivo cardiovascular and renal effects through WNK kinase inhibition.

靶点：

IC50: 5 nM (WNK1), 1 nM (WNK2), 6 nM (WNK3), and 9 nM (WNK4)

体内研究：

WNK463 (1-10 mg/kg；口服给药；4 小时；自发性高血压 Sprague Dawley 大鼠) 处理会在有意识的 SHR 中产生剂量依赖性血压降低和心率同步增加。WNK463 在尿量以及尿钠和尿钾排泄率方面产生显著的剂量依赖性增加。
WNK463 在 Sprague Dawley 大鼠体内具有口服生物利用度，半衰期为 2.1 小时。

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.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.158 ml	10.788 ml	21.577 ml
5 mM	0.432 ml	2.158 ml	4.315 ml
10 mM	0.216 ml	1.079 ml	2.158 ml
50 mM	0.043 ml	0.216 ml	0.432 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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