Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 963 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,420 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 578 | 现货 |
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 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50: 331 nM) and in recombinantly expressed h Nav1.8 channels (IC50: 196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50: 10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50: 10-18 μM). 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 [1]. |
体内活性 | PF-01247324 (100 mg/kg) reduces phase 2 flinching by 37%. There is a significant effect of 30 mg/kg of PF-01247324 in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively [1]. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control [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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (166.36 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.0248 mL | 15.124 mL | 30.248 mL | 75.6201 mL |
5 mM | 0.605 mL | 3.0248 mL | 6.0496 mL | 15.124 mL | |
10 mM | 0.3025 mL | 1.5124 mL | 3.0248 mL | 7.562 mL | |
20 mM | 0.1512 mL | 0.7562 mL | 1.5124 mL | 3.781 mL | |
50 mM | 0.0605 mL | 0.3025 mL | 0.605 mL | 1.5124 mL | |
100 mM | 0.0302 mL | 0.1512 mL | 0.3025 mL | 0.7562 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF-01247324 875051-72-2 Membrane transporter/Ion channel Sodium Channel PF01247324 PF 01247324 Na+ channels Na channels Inhibitor inhibit inhibitor