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PF01247324是一种选择性的、口服有效的Nav1.8通道阻断物,对人类重组Nav1.8 的IC50为196 nM。


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PF01247324是一种选择性的、口服有效的Nav1.8通道阻断物,对人类重组Nav1.8 的IC50为196 nM。
| 规格 | 价格 | 库存 | 数量 | 
|---|---|---|---|
| 1 mg | ¥ 148  | In stock | |
| 5 mg | ¥ 347  | In stock | |
| 10 mg | ¥ 578  | In stock | |
| 25 mg | ¥ 1,190  | In stock | |
| 50 mg | ¥ 2,230  | In stock | |
| 100 mg | ¥ 3,250  | In stock | |
| 200 mg | ¥ 4,570  | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 347  | In stock | 
PF-01247324 相关产品
| 产品描述 | PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker (IC50: 196 nM).  | 
| 靶点活性 |  Nav1.8 channel:196 nM  | 
| 体外活性 | PF-01247324抑制人类背根神经节(DRG)神经元中的天然耐受河豚毒素(TTX-R)电流(IC50:331 nM)及重组表达的h Nav1.8通道(IC50:196 nM),对重组表达的TTX-R hNav1.5通道具有50倍选择性(IC50:10 μM),对TTX敏感(TTX-S)通道具有65-100倍选择性(IC50:10-18 μM)。体外电流钳测试显示,PF-01247324降低了大鼠和人类DRG神经元的兴奋性,并改变了动作电位的波形[1]。  | 
| 体内活性 | PF-01247324 (100 mg/kg) 通过减少第二阶段的抽动37%显示出其效果。在大鼠模型的卡拉胶诱导的热痛觉过敏和CFA诱导的机械痛觉过敏实验中,30 mg/kg的PF-01247324分别在0.218和0.126 μM的浓度下表现出显著效果[1]。相较于对照组,接受PF-01247324处理的小鼠在运动协调性和类小脑症状方面有明显改善[2]。  | 
| 动物实验 | Rats: . For male Sprague Dawley rats (170-300?g), PF-01247324 is formulated as solutions of 0, 10, 30, 100?mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioral testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted[1]. Mice: . PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of the vehicle[2].  | 
| 分子量 | 330.6 | 
| 分子式 | C13H10Cl3N3O | 
| CAS No. | 875051-72-2 | 
| Smiles | CNC(=O)c1ccc(c(N)n1)-c1cc(Cl)cc(Cl)c1Cl | 
| 密度 | 1.460 g/cm3 (Predicted) | 
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 55 mg/mL (166.36 mM), Sonication is recommended.   | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.05 mM), Sonication is recommended.  请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表  | ||||||||||||||||||||||||||||||||||||
DMSO 
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