WNK463|cas:2012607-27-9|西域试剂

WNK463,99.07%

产品编号：Bellancom-100626| CAS NO：2012607-27-9| 分子式：C₂₁H₂₄F₃N₇O₂| 分子量：463.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100626	￥500.00	杭州北京（现货）
Bellancom-100626	￥1000.00	杭州北京（现货）
Bellancom-100626	￥1600.00	杭州北京（现货）
Bellancom-100626	￥3400.00	杭州北京（现货）
Bellancom-100626	￥5440.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

WNK463

产品介绍

WNK463 是一种口服的 WNK 激酶抑制剂，对于WNK1，WNK2，WNK3 和 WNK4 的 IC₅₀ 值分别为 5 nM，1 nM，6 nM 和 9 nM。

生物活性

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC_50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	Human tissue-engineered corneas (hTECs)
Concentration:	50 nM, 1 μΜ, 10 μΜ
Incubation Time:	6 days
Result:	Reduced phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age)
Dosage:	1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
Administration:	Oral administration; 4 hours
Result:	Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age)
Dosage:	1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
Administration:	Oral administration; 4 hours
Result:	Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age)
Dosage:	1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
Administration:	Oral administration; 4 hours
Result:	Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (64.73 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1577 mL	10.7884 mL	21.5768 mL
5 mM	0.4315 mL	2.1577 mL	4.3154 mL
10 mM	0.2158 mL	1.0788 mL	2.1577 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。