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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-IDOR-1104-0086
IDOR-1104-0086

Chemical Structure : IDOR-1104-0086

CAS No.: 2756581-81-2

IDOR-1104-0086

货号: PC-25451Not For Human Use, Lab Use Only.

IDOR-1104-0086 is a potent activator of Kv7.2/3 channels with EC50 of 192 nM in HEK293 cells stably expressing hKv7.2/3 heterotetramers (Emax=94%), and EC50 of 321 nM for hKv7.3/5 heterotetramers (Emax=85%).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IDOR-1104-0086 is a potent activator of Kv7.2/3 channels with EC50 of 192 nM in HEK293 cells stably expressing hKv7.2/3 heterotetramers (Emax=94%), and EC50 of 321 nM for hKv7.3/5 heterotetramers (Emax=85%).
IDOR-1104-0086 is more potent than retigabine on brain specific Kv7 channel isoforms.
IDOR-1104-0086 resulted in concentration-dependent increase in Tl+ flux with an EC50 of 199 nM and an Emax of 78 % in HEK293 cells stably expressing hKv7.2, which is >13-fold more potent than retigabine, also shows no species differences for rat Kv7.2.
IDOR-1104-0086 shows no effect on hKv7.1-expressing cells, and hKv7.5 homotetramer expressing cells.
IDOR-1104-0086 (3-30 mg/kg) reduced seizure activity in the amygdala-kindling rat model.

物理化学性质&存储条件

分子量 334.29
分子式 C15H15F5N2O
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

1-(3-(difluoromethyl)bicyclo[1.1.1]pentan-1-yl)-3-(3-(trifluoromethyl)benzyl)urea

参考文献

1. Kessler M, et al. Neuropharmacology. 2025 Aug 25;280:110658.

2. Siegrist R, et al. J Med Chem. 2025 Aug 28;68(16):17412-17426.

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