PF-05089771

PF-05089771用途

PF-05089771是一种有效的,状态依赖性的亚型选择性Nav1.7抑制剂,IC50为11 nM,选择性比Nav1.3,1.4和Nav1.5,1.8高1000倍；与域IV的电压传感器域(VSD)相互作用,阻断所有具有相似效力的Nav1.7剪接变体(5N11L,5A11S,5A11L和5N11S,IC50=11=33nM)；显示出对L型钙通道,KvLQT和hERG钾通道的高选择性；在小鼠辣椒素诱导的神经源性眩光模型中显示体内功效。疼痛阶段1已停止

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PF-05089771名称

[ CAS 号 ]:
1430806-04-4

[ 中文名 ]:
PF-05089771

[ 英文名 ]:
PF 05089771

[英文别名 ]:

PF-05089771
PF-05089771 p-toluene sulfonate salt
MFCD30146405
Pf-05089771 Tosylate

PF-05089771生物活性

[ 描述 ]:

[参考文献]

References 1. Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042. 2. Theile JW, et al. Mol Pharmacol. 2016 Nov;90(5):540-548. 3. Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405. 4. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801. View Related Products by Target Sodium Channel Pain

PF-05089771物理化学性质

[ 分子式 ]:
C₁₈H₁₂Cl₂FN₅O₃S₂

[ 分子量 ]:
672.556

[ 精确质量 ]:
670.993652

[ 储存条件 ]:
-20°C，密闭，干燥

PF-05089771安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

PF-05089771文献

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.

PLoS ONE 11(4) , e0152405, (2016)

Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has ...

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