SML2809

WNK463

≥98% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₂₁H₂₄F₃N₇O₂
• CAS番号: 2012607-27-9
• 分子量: 463.46
• MDL番号: MFCD30489744
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C

詳細

生物化学的／生理学的作用

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.).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable