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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
ICA-27243 targets KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channels, acting as a selective opener. By opening these channels, it enhances the M-current, a voltage-gated potassium current that stabilizes neuronal membrane potential. This reduces neuronal excitability and contributes to its anticonvulsant effects. It binds to a novel voltage-sensor domain site.
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| ln Vitro |
Coadministration of XE-991 and Linopirdine, two M current inhibitors, can decrease the membrane potential hyperpolarization that ICA-27243 causes in human neuroblastoma cells (SH-SY5Y). In Chinese hamster ovary cells that stably express heteromultimeric KCNQ2/Q3 channels, ICA-27243 increases 86Rb+ efflux (EC50 = 0.2 μM) and whole-cell currents (EC50 = 0.4 μM). The hyperpolarization shift that occurs when KCNQ2/Q3 channels are activated is reliant on the channel activation voltage (V1/2 shift of -19 mV at 10 μM) [1].
In vitro, ICA-27243 induces a concentration-dependent increase in 86Rb+ efflux from CHO cells expressing KCNQ2/Q3 channels with an EC50 of 0.2 μM. It is a selective activator of the neuronal M current. It is less effective at activating KCNQ4 and KCNQ3/Q5. |
| ln Vivo |
In a mouse maximum electroshock epilepsy paradigm, ICA-27243 (1-100 mg/kg; oral; male CD-1 mice) exhibits anticonvulsant action (ED50 of 8.4 mg/kg) [1].
In vivo, ICA-27243 displays anticonvulsant activity in the mouse maximal electroshock model with an ED50 of 8.4 mg/kg. It is orally active. The compound has antiepileptic properties. Its efficacy in seizure models supports its potential in epilepsy research. |
| Enzyme Assay |
In vitro assays for ICA-27243 typically measure its effects on KCNQ2/Q3 channel activity. Electrophysiological techniques such as patch-clamp are used to measure potassium currents in cells expressing the channels. 86Rb+ efflux assays are also used to assess channel opening. EC50 values are determined from concentration-response curves.
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| Cell Assay |
Cellular assays for ICA-27243 are performed using CHO cells expressing KCNQ2/Q3 channels. Cells are treated with the compound, and 86Rb+ efflux is measured. Alternatively, membrane potential-sensitive dyes can be used to assess channel activity in a higher-throughput format.
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| Animal Protocol |
Animal/Disease Models: Male CD-1 mice, electric shock test [1]
Doses: 1-100 mg/kg Route of Administration: Oral Experimental Results:There was a dose-dependent increase in hindlimb extension latency, with an ED50 value of 8.4 mg/kg. In vivo animal studies with ICA-27243 are conducted in the mouse maximal electroshock epilepsy model. Male CD-1 mice are administered the compound orally at doses ranging from 1-100 mg/kg. The ability of the compound to prevent convulsions is assessed. The ED50 is calculated. |
| ADME/Pharmacokinetics |
ICA-27243 is orally active. Its molecular weight is 268.65 g/mol. For research use, it is typically dissolved in DMSO for in vitro studies and formulated in suitable vehicles for oral administration. Its half-life and metabolic profile have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for ICA-27243 are limited. In animal studies, the compound shows anticonvulsant activity at doses up to 100 mg/kg. No significant toxicity has been reported at the doses used for efficacy studies. The compound is intended for research use and should be handled with standard safety precautions.
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| References |
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| Additional Infomation |
ICA-27243 is a research compound used as a selective KCNQ2/Q3 potassium channel opener. It has antiepileptic and anticonvulsant properties and is orally active. The compound is a valuable tool for studying the role of KCNQ2/Q3 channels in neuronal excitability and epilepsy. It is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C12H7CLF2N2O
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| Molecular Weight |
268.65
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| Exact Mass |
268.021
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| CAS # |
325457-89-4
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| PubChem CID |
9903497
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| Appearance |
White to off-white solid powder
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| LogP |
3.649
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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 |
2
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| Heavy Atom Count |
18
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| Complexity |
306
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GDGUOCFTHNGPBK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H7ClF2N2O/c13-11-4-2-8(6-16-11)17-12(18)7-1-3-9(14)10(15)5-7/h1-6H,(H,17,18)
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| Chemical Name |
N-(6-chloropyridin-3-yl)-3,4-difluorobenzamide
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| Synonyms |
ICA27243 ICA 27243 ICA-27243
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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 (~930.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7223 mL | 18.6116 mL | 37.2232 mL | |
| 5 mM | 0.7445 mL | 3.7223 mL | 7.4446 mL | |
| 10 mM | 0.3722 mL | 1.8612 mL | 3.7223 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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