PF-01247324

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-01247324 是一种选择性、口服生物可利用的 Nav1.8 通道阻断剂 (IC50: 196 nM)。

PF-01247324 is a novel selective and orally bioavailable Nav 1.8 channel blocker, attenuates nociception and sensory neuron excitability.

PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50=331 nM) and in recombinantly expressed h Nav1.8 channels (IC50=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC50=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC50=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.

PF-01247324 | PF 01247324 | PF01247324

Others

Other Targets

Na(V1.8) channel

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875051-72-2

330.6

C13H10Cl3N3O

>98% (HPLC)

DMSO : ≥ 30 mg/mL; 90.74 mM

CNC(=O)c1ccc(c(N)n1)-c1cc(Cl)cc(Cl)c1Cl

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

(-20℃)

With Ice Pack

≥ 2 years