ICA604025
ICA604025 is a state-dependent inhibitor of human Nav1.9 voltage-gated sodium channel. ICA604025 exerts stronger inhibitory effects on activated/inactivated Nav1.9 than on resting closed Nav1.9, and serves as a tool for investigating the physiological functions of Nav1.9. ICA604025 is applicable to pain-related research.
For research use only. We do not sell to patients.
- Formula: C16H15F5N2O3
- Molecular Weight:378.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Nav1.9 |
In Vitro
ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits human Nav1.9-5C channels in HEK-293 cells, with an EC50 of 9 nM for activated/inactivated states and 1.1 μM for resting closed states[1].
ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits wild-type human Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.76 μM for resting closed states[1].
ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits cynomolgus monkey Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.45 μM for resting closed states[1].
ICA604025 (0.001-100 μM; 4 minutes) inhibits mouse Nav1.9 channels in HEK-293 cells with an EC50 of 0.48 μM for activated/inactivated states, showing ~48-fold lower potency than for human Nav1.9[1].
ICA604025 (0.001-100 μM; 4 minutes) inhibits rat Nav1.9 channels in HEK-293 cells with an EC50 of 0.53 μM for activated/inactivated states, showing ~53-fold lower potency than for human Nav1.9[1].
ICA604025 (0.001-100 μM; 4 minutes) inhibits human Nav1.9-5CF1592A/Y1599A mutant channels in HEK-293 cells with an EC50 of 0.017 μM for activated/inactivated states, showing only a minor reduction in potency compared to wild-type Nav1.9-5C[1].
ICA604025 (0-10 μM) potently inhibits native Nav1.9 channels in human DRG neurons with an IC50 of 0.56 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 378.29
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Formula C16H15F5N2O3
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SMILES
O=C([C@H]1CN(CCO1)C2=CC3=C(C(C(F)(F)F)=CC=C3)O2)NCC(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- ICA604025
- ICA 604025
- ICA-604025
- Sodium Channel
- human Nav1.x family members
- human Nav1.9-5C channels
- human Nav1.9 voltage-gated sodium channel
- cynomolgus monkey Nav1.9 channels
- human DRG neuron channels
- rodent channels
- wild-type human Nav1.9 channels
- mouse Nav1.9 channels
- HEK-293 cells
- cynomolgus monkey channels
- Inhibitor
- inhibitor
- inhibit