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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-KCNQ2 activator Ebio1
KCNQ2 activator Ebio1

Chemical Structure : KCNQ2 activator Ebio1

CAS No.: 339287-36-4

KCNQ2 activator Ebio1 (Ebio1)

货号: PC-21613Not For Human Use, Lab Use Only.

KCNQ2 activator Ebio1 is a potent and subtype-selective activator for the voltage-gated potassium channel KCNQ2 (Kv7.2) with EC50 of 247.3 nM, directly opens the KCNQ2 channel.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KCNQ2 activator Ebio1 is a potent and subtype-selective activator for the voltage-gated potassium channel KCNQ2 (Kv7.2) with EC50 of 247.3 nM, directly opens the KCNQ2 channel.
Ebio1 (10  μM) dramatically caused up to 34.32 ± 2.00 mV left shift of the half-maximal activation voltage (V1/2), from −16.65 to −50.97 mV.
Ebio1 showed moderate activity for the KCNQ2/3, KCNQ4 and KCNQ5 channels, and negligible activation effects on Kv, NaV, CaV and K2P channel members, including hERG, BK, NaV1.1, CaV2.1 and TREK1.
Compared to the WT KCNQ2, the mutations W236A, L299A, I300A, S303A and F305A substantially decreased the potency of Ebio1.
Ebio1 activates KCNQ2 via a twist-to-open mechanism.

物理化学性质&存储条件

分子量 291.33
分子式 C19H14FNO
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-(1,2-dihydroacenaphthylen-5-yl)-4-fluorobenzamide

参考文献

1. Shaoying Zhang, et al. Nat Chem Biol. 2024 Jan 2. doi: 10.1038/s41589-023-01515-y.

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