货号	规格	价格	上海	北京	珠海	重庆	武汉
S86978-5mg	≥98%	￥433.00 S86978-5mg ￥433.00 3-5天	0 货期：3-5天	-	-	-	-
S86978-10mg	≥98%	￥722.00 S86978-10mg ￥722.00 3-5天	0 货期：3-5天	-	-	-	-
S86978-25mg	≥98%	￥1487.00 S86978-25mg ￥1487.00 3-5天	0 货期：3-5天	-	-	-	-
S86978-50mg	≥98%	￥2468.00 S86978-50mg ￥2468.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel

靶点：

IC50: 196 nM (hNav1.8);SodiumChannel

体外研究：

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

体内研究：

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

参考文献：

1. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. 2. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.025 ml	15.124 ml	30.248 ml
5 mM	0.605 ml	3.025 ml	6.05 ml
10 mM	0.302 ml	1.512 ml	3.025 ml
50 mM	0.06 ml	0.302 ml	0.605 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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