Chemical Structure : IDOR-1104-0086
CAS No.:
2756581-81-2
IDOR-1104-0086
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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334.29
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Formula
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C15H15F5N2O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(3-(difluoromethyl)bicyclo[1.1.1]pentan-1-yl)-3-(3-(trifluoromethyl)benzyl)urea
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References
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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