2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
中文名称 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - |
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中文同义词 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -;化合物PF01247324;6-氨基-N-甲基-5-(2,3,5-三氯苯基)吡啶-2-甲酰胺 |
英文名称 | PF-01247324 |
英文同义词 | 2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-;6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide;6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE;PF-1247324;PF-01247324;6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE;PF01247324;PF 01247324;133786 |
CAS号 | 875051-72-2 |
分子式 | C13H10Cl3N3O |
分子量 | 330.6 |
EINECS号 | |
相关类别 | |
Mol文件 | 875051-72-2.mol |
结构式 |
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - 性质
沸点 | 477.7±45.0 °C(Predicted) |
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密度 | 1.460±0.06 g/cm3(Predicted) |
储存条件 | room temp |
溶解度 | DMF:30mg/mL; DMSO:30mg/mL;乙醇:30mg/mL;乙醇:PBS (pH 7.2) (1:4): 0.2 mg/mL |
酸度系数(pKa) | 6.56±0.46(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
IC50: 196 nM (hNa v 1.8)
PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC 50 =331 nM) and in recombinantly expressed h Na v 1.8 channels (IC 50 =196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC 50 =10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC 50 =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.
Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models. PF-01247324 reduces phase 2 flinching by 37% at 100 mg/kg. 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. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control.
安全信息
危险品运输编号 | UN 2811 6.1 / PGIII |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-101383 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - PF-01247324 | 875051-72-2 | 5mg | 700元 |
2024/08/19 | HY-101383 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - PF-01247324 | 875051-72-2 | 10mM * 1mLin DMSO | 770元 |