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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-Compound 1028
Compound 1028

Chemical Structure : Compound 1028

CAS No.: 3065963-83-6

Compound 1028 (FGF14/Nav1.6 modulator)

货号: PC-23790Not For Human Use, Lab Use Only.

Compound 1028 is a potent, brain-permeable small molecule that targets FGF14 R117 with binding KD of 293 nM (SPR), selectively modulates FGF14/Nav1.6 complex assembly and depolarizes the voltage-dependence of Nav1.6 channel inactivation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Compound 1028 is a potent, brain-permeable small molecule that targets FGF14 R117 with binding KD of 293 nM (SPR), selectively modulates FGF14/Nav1.6 complex assembly and depolarizes the voltage-dependence of Nav1.6 channel inactivation.
Compound 1028 shows no detectable binding to the Nav1.6 CTD, but modulates the intramolecular interaction between the III-IV linker and C-terminal domain of the Nav1.6 channel.
Compound 1028 (1 uM) caused a depolarizing shift in the voltage-dependence of steady-state inactivation of INa in HEK293 cells transiently transfected with Nav1.6WT and FGF14.
Compound 1028 shows no effect on the voltage-dependence of steady-state inactivation of INa in HEK293 cells expressing Nav1.1 and FGF14 or Nav1.2 and FGF14.
Compound 1028 enhances medium spiny neurons (MSN) excitability ex vivo and accumbal neuron firing rate in vivo in murine models, displays behavioral motivation preferentially during motivationally deficient conditions.

物理化学性质&存储条件

分子量 352.39
分子式 C20H20N2O4
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

ethyl 3-(2-(3-(hydroxymethyl)-1H-indol-1-yl)acetamido)benzoate

参考文献

1. Dvorak NM, et al. Nat Commun. 2025 Jan 2;16(1):110.

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