WNK-IN-11|2123489-30-3|-陌孚医药/Medlife

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WNK-IN-11

目录号: PL11232 纯度: ≥99%

CAS No. :2123489-30-3

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中文名称	WNK-IN-11
英文名称	WNK-IN-11
英文别名	(5-Chloro-2-(2-(methylamino)thiazol-4-yl)pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone;WNK Inhibitor 11;BCP32643;BDBM50258566;ClC=1C(=CC(=NC=1)C=1N=C(SC=1)NC)C(=O)N1CCN(CC1)CC1=CC=C(C=C1)Cl;Wnk-IN-11;WNK-IN-11
Cas No.	2123489-30-3
分子式	C₂₁H₂₁Cl₂N₅Os
分子量	462.40
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	WNK-IN-11 是 (WNK) 激酶的变构抑制剂，其对 WNK1 的IC₅₀ 值为 4 nM。
生物活性	WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC 50 of 4 nM for WNK1.
性状	Solid
IC50 & Target[1][2]	IC50: 4 nM (WNK1).
体外研究(In Vitro)	WNK-IN-11 (compound 11) shows IC50<2 μM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility, albeit with still rather high microsomal clearance. WNK-IN-11 shows ATP noncompetitive inhibition. When tested against a panel of 440 human kinases at 10 μM concentration, 2500-fold above enzyme IC50 value, WNK-IN-11 shows excellent selectivity with only a few significant off-target kinase inhibitions, most notably BTK and feline encephalitis virus-related (FER) kinase, neither of which are implicated for blood pressure regulation. This excellent selectivity profile is consistent with the predicted allosteric binding mode outside the highly conserved ATP-pocket. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献	[1]. Yamada K, et al. Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models. J Med Chem. 2017 Aug 24;60(16):7099-7107.

溶解度数据	In Vitro: DMSO : 150 mg/mL (324.39 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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