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PF 05089771,Nav1.7通道阻滞剂

    
≥98%(HPLC)

4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-benzenesulfonamide Tosylate

源叶(MedMol)
T23129 一键复制产品信息
1430806-04-4
C25H20Cl2FN5O6S3
672.5556032
PF 05089771 Tosylate;PF-05089771 (tosylate)
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T23129-5mg促销
≥98%(HPLC)

¥1020.00 ¥920.00

10 - - - -
T23129-10mg促销
≥98%(HPLC)

¥1770.00 ¥1590.00

10 - - - -
T23129-25mg促销
≥98%(HPLC)

¥4070.00 ¥3670.00

5 - - - -
T23129-50mg促销
≥98%(HPLC)

¥7130.00 ¥6420.00

2 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: PF 05089771 tosylate 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) 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.
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.487 ml 7.434 ml 14.869 ml
5 mM 0.297 ml 1.487 ml 2.974 ml
10 mM 0.149 ml 0.743 ml 1.487 ml
50 mM 0.03 ml 0.149 ml 0.297 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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