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PF-01247324  ≥98%

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥430mg/ml)
产品描述：基本信息 产品编号： P11303  产品名称： PF-01247324 CAS: 875051-72-2   储存条件 粉末 -20℃ 四年     分子式： C13H10Cl3N3O 溶于液体 -80℃ 6个月 分子量： 330.60 -20℃ 1个月 化学名：  6-amino-N-methyl-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.0248mL 15.1240mL 30.2480mL 5mM 0.6050mL 3.0248mL 6.0496mL 10mM 0.3025mL 1.5124mL 3.0248mL   生物活性 产品描述 一种选择性的且有口服活性的Nav1.8通道阻断物，对人类重组Nav1.8的IC50值为196nM。 靶点 IC50:196nM (hNav1.8)   体外研究 PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50=331nM) and in recombinantly expressed h Nav1.8 channels (IC50=196nM),with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50=10μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50=10-18μM).In vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential. 体内研究 Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models.PF-01247324 reduces phase 2 flinching by 37% at 100mg/kg.There is a significant effect of 30mg/kg of PF-01247324 in the rat model carrageenaninduced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126μM respectively.Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control.   推荐实验方法(仅供参考) 动物实验:   Rats:For male Sprague Dawley rats (170-300g),PF-01247324 is formulated as solutions of 0,10,30,100mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural 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. Mice:PF-01247324 is suspended in 0.5% methylcellulose,0.1% Tween 80 and administered by oral gavage at a dose of 1000mg/kg in a volume of 10mL/kg one hour before behavioral testing.Control groups are administered an equal volume of vehicle.
保存条件：-20℃

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