| CAS: | 2012607-27-9 | |
| 分子式: | C21H24F3N7O2 | |
| 分子量: | 463.46 | |
| 英文名称: |
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| 用途: | WNK463是一种WNK激酶的泛抑制剂。在体外实验中,它能有效地抑制WNK激酶家族中4个成员的活性(WNK1, WNK2, WNK3和WNK4) |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | 详情 | ||||||||||||||||||||||||||||
| W797375 | MACKLIN | WNK463 | 10mM in DMSO | 898元/1ml; | 展开 | ||||||||||||||||||||||||||||
储存:-20°C | |||||||||||||||||||||||||||||||||
| W872792 | MACKLIN | WNK463 | 99% | 999元/5mg; | 展开 | ||||||||||||||||||||||||||||
储存:-20℃ 状态:粉末 | |||||||||||||||||||||||||||||||||
| SML2809 | Sigma-Aldrich | WNK463 | ≥98% (HPLC) | 1045.52元/5 MG; 4001.66元/25 MG; | 展开 | ||||||||||||||||||||||||||||
产品说明 生化/生理作用 WNK463 is a high-affinity, ATP-competitive inhibitor against with-No-Lysine (K) kinases (hWNK1/3/4 IC50 = 5/6/9 nM with MBP & 1 μM ATP, hWNK2 IC50 = 1 nM with MBP & 2 μM ATP, hWNK1 IC50 = 41 nM with OSR1 & 0.5 μM ATP; hWNK1/4 KD = 3.71/3.84 by SPR), exhibiting weak affinity against only two other human kinases among a panel of 442. WNK463 downregulates the overexpressed OSR1 phosphorylation level in HEK293 cells (IC50 = 106 nM; 1 hr) and displays in vivo efficacy in rodent hypertension models (1-10 mg/kg in rats p.o., 10 mg/kg in hWNK1 transgenic mice p.o.) with good orally availability (F = 100%/mice & 74%/rats post 1.5 mg/kg p.o.). 基本信息
产品性质
安全信息
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