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)-kinaseinhibitor withIC50sof 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively[1]. |
IC50& Target | IC50: 5 nM (WNK1), 1 nM (WNK2), 6 nM (WNK3), and 9 nM (WNK4)[1] |
体外研究 (In Vitro) | 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.
Western Blot Analysis[2] 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. |
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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[1].
Animal Model: | Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age)[1] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 30 mg/mL(64.73 mM) *"≥" means soluble, but saturation unknown. 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 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。 *以上所有助溶剂都可在本网站选购。
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