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WNK463

产品编号:4086467
规格:≥98% (HPLC)
CAS NO:2012607-27-9
包装规格:5 MG,25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
40864675 MG1150
408646725 MG4000
产品别名

2012607-27-9

WNK463

N-(1,1-Dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-1H-imidazole-5-carboxamide

N-tert-Butyl-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-4-yl)-1H-imidazole-5-carboxamide

结构式
基本信息
Empirical Formula【经验(实验)分子式】
C21H24F3N7O2
Molecular weight
463.46
MDL number
MFCD30489744
Biochem/physiol Actions【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.).
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
powder
color【颜色】
white to beige
solubility【溶解性】
DMSO: 2 mg/mL, clear
storage temp.【储存温度】
2-8℃
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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