E0199

Chemical Structure : E0199

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货号: PC-24070Not For Human Use, Lab Use Only.

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生物&药学活性

E0199 is a dual-targeting inhibitor of NaV1.7, NaV1.8, and NaV1.9 and activator of KV7 channels with IC50 of 0.52 uM (NaV1.7), 0.24 uM (NaV1.8), 0.16 uM (NaV1.9), and EC50 of 0.5 uM/12.78 nM/0.19 uM for KV7.2, KV7.2/7.3 and KV7.4 channels.
E0199 (10 μM) could inhibit NaV currents with different ability, and the inhibition rates of NaV1.5, NaV1.4, NaV1.1, NaV1.6, NaV1.7, NaV1.8, and NaV1.9 channels were 15.00% ± 6.90%, 1.07% ± 3.16%, 0.56% ± 1.14%, 1.17% ± 3.16%, 57.53% ± 4.50%, 75.33% ± 7.96%, and 46.82% ± 7.03%, respectively.
The sequence of NaV channel inhibition of E0199 at 10 μM was NaV1.8 > NaV1.7 > NaV1.9 > NaV1.5 > NaV1.6 > NaV1.4 > NaV1.1.
The order activation of KV7 channel is KV7.2/7.3 > KV7.2 > KV7.5 > KV7.4
E0199 significantly reduced the excitability of dorsal root ganglion neurons and alleviated pain hypersensitivity in mice.

物理化学性质&存储条件

分子量	535.65
分子式	C29H37N5O5
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N-benzyl-3-(3-((4-(2-(3,4-dimethoxyphenyl)acetyl)piperazin-1-yl)methyl)-1,2,4-oxadiazol-5-yl)-N-ethylpropanamide

参考文献

1. Zhang B, et al. J Pharm Anal. 2025 Jan;15(1):101132.

E0199

生物&药学活性

物理化学性质&存储条件

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E0199

生物&药学活性

物理化学性质&存储条件

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