875051-72-2
基本信息
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
CS-2577
PF-1247324
PF-01247324
PF01247324
PF 01247324
6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide
6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE
2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-
6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE
物理化學(xué)性質(zhì)
報(bào)價(jià)日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
2024/11/08 | 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 |
2024/11/08 | 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 |
2024/11/08 | 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 | 10mg | 1200元 |
常見問題列表
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.