货号	规格	价格	上海	北京	珠海	重庆	武汉
S82522-1mg	≥98%	￥239.00 S82522-1mg ￥239.00 现货	8 0 8	-	-	-	-
S82522-5mg	≥98%	￥489.00 S82522-5mg ￥489.00 现货	7 0 7	-	-	-	-
S82522-10mg	≥98%	￥739.00 S82522-10mg ￥739.00 现货	3 0 3	-	-	-	-
S82522-25mg	≥98%	￥1460.00 S82522-25mg ￥1460.00 现货	1 1	-	-	-	-
S82522-50mg	≥98%	￥2490.00 S82522-50mg ￥2490.00 现货	2 2	-	-	-	-

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产品描述：

PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

靶点：

IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7);SodiumChannel

体外研究：

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4) PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5, Fig 5D) whilst 100 nM resulted in complete block

参考文献：

1. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. 2. Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.999 ml	9.993 ml	19.986 ml
5 mM	0.4 ml	1.999 ml	3.997 ml
10 mM	0.2 ml	0.999 ml	1.999 ml
50 mM	0.04 ml	0.2 ml	0.4 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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