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875051-72-2

中文名稱 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
英文名稱 PF-01247324
CAS 875051-72-2
分子式 C13H10Cl3N3O
分子量 330.6
MOL 文件 875051-72-2.mol
更新日期 2026/07/13 13:11:17
875051-72-2 結構式 875051-72-2 結構式

基本信息

中文別名
化合物PF01247324
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
英文別名
133786
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
所屬類別
生物化工:激動劑抑制劑

物理化學性質

沸點477.7±45.0 °C(Predicted)
密度1.460±0.06 g/cm3(Predicted)
儲存條件room temp
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
酸度系數(shù)(pKa)6.56±0.46(Predicted)
形態(tài)粉末
顏色白色至米色
InChI1S/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)
InChIKeyHPIUHDCRVYDAEJ-UHFFFAOYSA-N
SMILESClc1c(cc(cc1c2c(nc(cc2)C(=O)NC)N)Cl)Cl

安全數(shù)據(jù)

危險性符號(GHS)有毒 (GHS06)
GHS06
警示詞危險
危險性描述H301-H315-H319-H335
危險品運輸編號UN 2811 6.1 / PGIII
WGK GermanyWGK 3
存儲類別6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects
危險性類別Acute Tox. 3 Oral
Eye Irrit. 2
Skin Irrit. 2
STOT SE 3
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-1013832 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
PF-01247324
875051-72-25mg700元
2026/06/05HY-1013832 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
PF-01247324
875051-72-210mM * 1mLin DMSO770元
2026/06/05HY-1013832 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
PF-01247324
875051-72-210mg1200元

常見問題列表

生物活性
PF-01247324是選擇性且有口服活性的Nav1.8通道阻斷物,對人類重組Nav1.8 的IC50值為196 nM。
靶點

IC50: 196 nM (hNa v 1.8)

體外研究

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.

體內研究

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.

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