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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-PW164
PW164

Chemical Structure : PW164

CAS No.: 2459268-10-9

PW164 (PW-164)

货号: PC-25069Not For Human Use, Lab Use Only.

PW164 is a specific, small molecule inhibitor of FGF13/Nav1.7 channel C-terminal tail domain (CTD) PPI interface with IC50 of 29 uM (FGF13/Nav1.7 complex assembly), selectively modulates Nav1.7 currents.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PW164 is a specific, small molecule inhibitor of FGF13/Nav1.7 channel C-terminal tail domain (CTD) PPI interface with IC50 of 29 uM (FGF13/Nav1.7 complex assembly), selectively modulates Nav1.7 currents.
PW164 selectively suppresses capsaicin-induced signaling in hIPSC-derived sensory neurons.
PW164 displays appreciable binding for FGF13 (KD of 21 μM) but shows no interaction with Nav1.7 CTD.
PW164 reverses FGF13-induced increase in INa density dose dependently, with an IC50 of 6.74 μM and induces LTI while decelerating Nav1.7 repriming.
PW164 is an FGF13-dependent analgesic that preserves normal sensory function, exerts antinociceptive effects and mimics in vivo FGF13 knockdown.
PW164 (15 mg/kg, i.d.) reduces mechanical hyperalgesia in the HFD-induced T2DN mouse model.

物理化学性质&存储条件

分子量 660.81
分子式 C34H52N4O9
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

benzyl (S)-2-(((S)-1-(((S)-5-(tert-butoxy)-1-(((S)-1-methoxy-3-methyl-1-oxobutan-2-yl)amino)-1,5-dioxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)carbamoyl)pyrrolidine-1-carboxylate

参考文献

1. Singh AK, et al. J Clin Invest. 2025 Jul 15;135(14):e183749.

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