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| 10mg |
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| Targets |
ICA-105574 targets the hERG potassium channel (Kv11.1), which plays a critical role in the repolarization of the cardiac action potential. It acts as a channel activator by binding to the channel and removing its inactivation. This increases the peak current amplitude and shortens the action potential duration. The compound has an EC50 of 0.5 μM for potentiating hERG channel activity. It also modulates the channel's activation kinetics.
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| ln Vitro |
ICA-105574 is a potent and efficacious hERG channel activator that steeply potentiates current amplitudes more than 10-fold with an EC50 of 0.5 μM. The primary mechanism by which it potentiates hERG channel activity is by removing hERG channel inactivation. It also modulates channel activation kinetics and shortens the action potential. Its activity has been confirmed in various electrophysiological assays.
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| ln Vivo |
ICA-105574 enhances peak current and shortens action potential duration in cardiac cells. Its ability to activate hERG channels and shorten the action potential could have implications for cardiac electrophysiology. However, detailed in vivo efficacy data in animal models is limited. The compound is primarily used as a research tool to study hERG channel function and cardiac electrophysiology.
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| Enzyme Assay |
The primary in vitro assay for ICA-105574 is electrophysiological recording using the patch-clamp technique. hERG channels are expressed in cells such as CHO or HEK293 cells, and the compound's effects on channel currents are measured. The potentiation of current amplitude and the removal of inactivation are assessed. The EC50 of 0.5 μM is determined from dose-response curves.
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| Cell Assay |
In vitro cellular experiments for ICA-105574 involve treating cells expressing hERG channels with the compound and measuring its effects on channel activity using patch-clamp electrophysiology. The effects on action potential duration can be assessed in cardiomyocytes or other excitable cells. The compound's effects on channel gating and kinetics are analyzed.
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| Animal Protocol |
In vivo animal experiments for ICA-105574 are not extensively detailed in the available literature. As a hERG channel activator, it could be evaluated in animal models of cardiac arrhythmias or long QT syndrome. Its effects on cardiac electrophysiology and arrhythmia susceptibility would be assessed. Its pharmacokinetic properties and safety profile would also be evaluated.
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| ADME/Pharmacokinetics |
ICA-105574 has a molecular weight of 334.33 g/mol and a molecular formula of C19H14N2O4. It has a purity of ≥98%. It is soluble in DMSO. It is typically used as a research reagent and is stored as a powder at -20°C for long-term stability. It is also known as 3-nitro-N-(4-phenoxyphenyl)benzamide.
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| Toxicity/Toxicokinetics |
ICA-105574 is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As with all research chemicals, standard safety precautions should be followed when handling. Its safety would need to be established for therapeutic applications.
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| References | |
| Additional Infomation |
ICA-105574 is a potent and highly efficacious activator of the hERG potassium channel (Kv11.1). It enhances hERG channel activity by removing channel inactivation and steeply potentiates current amplitudes more than 10-fold with an EC50 of 0.5 μM. ICA-105574 also modulates channel activation kinetics and shortens the action potential. It is used in research on hERG channel function and cardiac electrophysiology.
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| Molecular Formula |
C19H14N2O4
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|---|---|
| Molecular Weight |
334.33
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| Exact Mass |
334.095
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| CAS # |
316146-57-3
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| PubChem CID |
715924
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.235
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GDWKBKTVROCPNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14N2O4/c22-19(14-5-4-6-16(13-14)21(23)24)20-15-9-11-18(12-10-15)25-17-7-2-1-3-8-17/h1-13H,(H,20,22)
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| Chemical Name |
3-nitro-N-(4-phenoxyphenyl)benzamide
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| Synonyms |
ICA105574; ICA 105574; ICA-105574
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~747.76 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9911 mL | 14.9553 mL | 29.9106 mL | |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9821 mL | |
| 10 mM | 0.2991 mL | 1.4955 mL | 2.9911 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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