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ICA 110381 (Compound 16) is a potent KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/Q3 agonist (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).
| Targets |
ICA 110381 targets KCNQ2/Q3 potassium channels (EC₅₀ = 0.3 μM for KCNQ2/Q3 heteromeric channels) [1]
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|---|---|
| ln Vitro |
- KCNQ2/Q3 channel activation: ICA 110381 potently activated KCNQ2/Q3 heteromeric channels expressed in CHO cells, with an EC₅₀ of 0.3 μM; it shifted the voltage dependence of channel activation to more negative potentials (-15 mV at 1 μM) and increased the maximum current amplitude by 2.8-fold at 10 μM [1]
- Selectivity: ICA 110381 showed minimal activity on KCNQ1, KCNQ4, KCNQ5, and other potassium channels (IC₅₀ > 10 μM for KCNQ1), demonstrating high selectivity for KCNQ2/Q3 channels [1] - Neuronal excitability modulation: In cultured rat hippocampal neurons, ICA 110381 (0.1-1 μM) dose-dependently reduced action potential firing frequency by 40-70% and prolonged the afterhyperpolarization phase, without affecting resting membrane potential [1] |
| ln Vivo |
- Anticonvulsant activity: In the mouse maximal electroshock seizure (MES) model, ICA 110381 administration (10, 30 mg/kg, intraperitoneal injection) dose-dependently inhibited seizures, with ED₅₀ values of 18 mg/kg; 30 mg/kg dose protected 80% of mice from tonic-clonic seizures [1]
- Pentylenetetrazole (PTZ)-induced seizure model: ICA 110381 (20 mg/kg, intraperitoneal injection) significantly increased the latency to first seizure by 95% and reduced the seizure severity score from 4.2 to 1.8 compared to vehicle control [1] |
| Enzyme Assay |
- Patch-clamp electrophysiology assay: CHO cells stably expressing human KCNQ2/Q3 heteromeric channels were cultured and plated on glass coverslips; whole-cell patch-clamp recordings were performed in a bath solution containing ICA 110381 (0.01-10 μM) [1]
Voltage steps from -80 mV to +40 mV (10 mV increments, 500 ms duration) were applied to evoke channel currents; current-voltage relationships and activation curves were analyzed to determine EC₅₀ values and voltage shift effects [1] - Selectivity assay: Patch-clamp recordings were also conducted on CHO cells expressing KCNQ1, KCNQ4, KCNQ5, or hERG channels, with ICA 110381 (0.1-10 μM) added to the bath solution to evaluate cross-reactivity [1] |
| Cell Assay |
- Hippocampal neuron excitability assay: Primary rat hippocampal neurons were cultured for 14-21 days, then ICA 110381 (0.1-1 μM) was added to the culture medium [1]
Whole-cell patch-clamp recordings were used to measure action potential firing rate, resting membrane potential, and afterhyperpolarization amplitude following current injection (50-200 pA, 500 ms) [1] |
| Animal Protocol |
- Maximal Electroshock Seizure (MES) model: Male CD-1 mice (20-25 g) were randomly divided into treatment and control groups (n=8 per group); ICA 110381 (10, 30 mg/kg) was administered via intraperitoneal injection 30 minutes before MES induction (50 mA, 0.2 seconds, corneal electrodes) [1]
Seizure severity was scored (0 = no seizure, 5 = fatal tonic-clonic seizure), and ED₅₀ was calculated by probit analysis [1] - PTZ-induced seizure model: Mice were treated with ICA 110381 (20 mg/kg, intraperitoneal injection) 30 minutes before PTZ administration (85 mg/kg, subcutaneous injection); latency to first seizure, seizure duration, and severity score were recorded for 30 minutes [1] Drug formulation: ICA 110381 was dissolved in DMSO (10% v/v) and diluted with saline to the final working concentration, with DMSO final concentration ≤1% [1] |
| References | |
| Additional Infomation |
ICA 110381 is a synthetic small molecule belonging to the N-pyridylbenzamide class [1]. Its anticonvulsant mechanism involves the activation of KCNQ2/Q3 potassium channels, which are highly expressed in the central nervous system and play a key role in regulating neuronal excitability [1]. ICA 110381 inhibits excessive neuronal firing by enhancing KCNQ2/Q3-mediated M currents, which is one of the core pathophysiological features of epilepsy [1]. The compound has good potency and selectivity for KCNQ2/Q3 channels, making it a potential drug for the treatment of epilepsy [1].
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| Molecular Formula |
C12H8CL2N2O
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|---|---|
| Molecular Weight |
267.11072063446
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| Exact Mass |
266.001
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| CAS # |
325457-99-6
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| PubChem CID |
4314115
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| Appearance |
White to off-white solid powder
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| LogP |
3.713
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FOYOGIUAMYSVIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H8Cl2N2O/c13-9-3-1-8(2-4-9)12(17)16-10-5-6-11(14)15-7-10/h1-7H,(H,16,17)
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| Chemical Name |
4-chloro-N-(6-chloropyridin-3-yl)benzamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.7438 mL | 18.7189 mL | 37.4378 mL | |
| 5 mM | 0.7488 mL | 3.7438 mL | 7.4876 mL | |
| 10 mM | 0.3744 mL | 1.8719 mL | 3.7438 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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