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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-ICA00600232
ICA00600232

Chemical Structure : ICA00600232

CAS No.:

ICA00600232 (ICA-00600232)

货号: PC-25532Not For Human Use, Lab Use Only.

ICA00600232 is a potent, selective small molecule Nav1.1 sodium channel potentiator with EC50 of 24 nM, exhibits >1000-fold selectivity for human Nav1.1 over all other Nav1.x family members except Nav1.3 (EC50=98 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ICA00600232 is a potent, selective small molecule Nav1.1 sodium channel potentiator with EC50 of 24 nM, exhibits >1000-fold selectivity for human Nav1.1 over all other Nav1.x family members except Nav1.3 (EC50=98 nM).
ICA00600232 displays comparative EC50s for Nav1.1 potentiation for rodents (mouse and rat), dog, pig, and nonhuman primates (marmoset and cynomolgus monkey), with 2- to 5-fold different from the 24 nM (human Nav1.1).
ICA00600232 (1 uM) produces an 11 mV depolarizing shift in voltage-dependence of activation of human Nav1.1 and a larger 23 mV depolarizing shift in voltage-dependence of steady-state inactivation.
ICA00600232 interacts with homologous domain 4 of Nav1.1.
ICA00600232 (10 nM-1 uM) increases excitability of cortical interneurons from scn1a+/− and wild-type mice.

物理化学性质&存储条件

分子量 451.48
分子式 C24H23F2N5O2
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

N-(4-(2,5-difluorophenyl)-6-(2-oxa-6-azaspiro[3.3]heptan-6-yl)pyrimidin-5-yl)-6-isopropyl nicotinamide

参考文献

1. Gallucci A, et al. Mol Pharmacol. 2025 Aug 21;107(10):100072.

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