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ICA-105574 

Cat. No. M29900
ICA-105574  Structure
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Biological Activity

ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2.

Chemical Information
Molecular Weight 334.33
Formula C19H14N2O4
CAS Number 316146-57-3
Form Solid
Solubility (25°C) DMSO 250 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Eva-Maria Zangerl-Plessl, et al. J Chem Inf Model. Toward a Structural View of hERG Activation by the Small-Molecule Activator ICA-105574

[2] Jing Meng, et al. Eur J Pharmacol. Compound ICA-105574 prevents arrhythmias induced by cardiac delayed repolarization

[3] Vivek Garg, et al. Mol Pharmacol. ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels

[4] Mahoko Asayama, et al. J Pharmacol Sci. Effects of an hERG activator, ICA-105574, on electrophysiological properties of canine hearts

[5] Aaron C Gerlach, et al. Mol Pharmacol. Pharmacological removal of human ether-à-go-go-related gene potassium channel inactivation by 3-nitro-N-(4-phenoxyphenyl) benzamide (ICA-105574)

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Keywords: ICA-105574  supplier, Potassium Channel, inhibitors, activators

 
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