2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
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) |
|---|---|
| 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 |
| InChI | 1S/C13H10Cl3N3O/c1-18-13(20)10-3-2-7(12(17)19-10)8-4-6(14)5-9(15)11(8)16/h2-5H,1H3,(H2,17,19)(H,18,20) |
| InChIKey | HPIUHDCRVYDAEJ-UHFFFAOYSA-N |
| SMILES | Clc1c(cc(cc1c2c(nc(cc2)C(=O)NC)N)Cl)Cl |
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - 用途与合成方法
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 |
|---|---|
| WGK Germany | WGK 3 |
| 存储类别 | 6.1C - 可燃，急性毒性 类别3 毒性化合物或者引起慢性影响的化合物 |
| 危险性类别 | 急性毒性 类别3经口 眼部刺激 类别2 经皮刺激 类别2 特异性靶器官毒性-一次接触，类别3 |
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-06-05 | HY-101383 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - | 875051-72-2 | 5mg | 700 |
| 2026-06-05 | HY-101383 | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - | 875051-72-2 | 10mM * 1mLin DMSO | 770 |
