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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-PF-01247324
PF-01247324

Chemical Structure : PF-01247324

CAS No.: 875051-72-2

PF-01247324 (PF01247324, PF 01247324)

货号: PC-42355Not For Human Use, Lab Use Only.

PF-01247324 is a potent, selective and orally active Nav1.8 channel blocker with IC50 of 196 nM, inhibits native TTX-R currents in human DRG neurons with IC50 of 331 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-01247324 is a potent, selective and orally active Nav1.8 channel blocker with IC50 of 196 nM, inhibits native TTX-R currents in human DRG neurons with IC50 of 331 nM.
PF-01247324 displays >50-fold selectivity over Nav1.5, Nav1.2 and Nav1.7 channels.
PF-01247324 inhibits native TTX-R currents in small-diameter rodent DRG neurons with IC50 of 448 nM, reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential in vitro current clamp.
PF-01247324 demonstrates efficacy in both inflammatory and neuropathic pain models.

物理化学性质&存储条件

分子量 330.597
分子式 C13H10Cl3N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxamide, 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)-

参考文献

1. Payne CE, et al. Br J Pharmacol. 2015 May;172(10):2654-70.

2. Shields SD, et al. PLoS One. 2015 Mar 6;10(3):e0119067.

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