2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) -
| 中文名稱(chēng) | 2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - |
|---|---|
| 中文同義詞 | 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;化合物PF01247324,10 MM DMSO 溶液;TPF-0124732;PF-01247324 (PF01247324;PF 01247324) |
| 英文名稱(chēng) | PF-01247324 |
| 英文同義詞 | 2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-;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;CS-2577 |
| CAS號(hào) | 875051-72-2 |
| 分子式 | C13H10Cl3N3O |
| 分子量 | 330.6 |
| EINECS號(hào) | |
| 相關(guān)類(lèi)別 | |
| Mol文件 | 875051-72-2.mol |
| 結(jié)構(gòu)式 |  |
2 - 吡啶甲酰胺,6 - 氨基-N-甲基-5 - (2,3,5 - 三氯苯基) - 性質(zhì)
| 沸點(diǎn) | 477.7±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.460±0.06 g/cm3(Predicted) |
| 儲(chǔ)存條件 | 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 |
| 酸度系數(shù)(pKa) | 6.56±0.46(Predicted) |
| 形態(tài) | 粉末 |
| 顏色 | 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 |
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
| 危險(xiǎn)品運(yùn)輸編號(hào) | UN 2811 6.1 / PGIII |
|---|---|
| WGK Germany | WGK 3 |
| 存儲(chǔ)類(lèi)別 | 6.1C - 可燃，急性毒性 類(lèi)別3 毒性化合物或者引起慢性影響的化合物 |
| 危險(xiǎn)性類(lèi)別 | 急性毒性 類(lèi)別3經(jīng)口 眼部刺激 類(lèi)別2 經(jīng)皮刺激 類(lèi)別2 特異性靶器官毒性-一次接觸，類(lèi)別3 |
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)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) - PF-01247324 | 875051-72-2 | 5mg | 700元 |
| 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) - PF-01247324 | 875051-72-2 | 10mM * 1mLin DMSO | 770元 |