ICA 110381
Based on 1 Customer Validation
ICA 110381 is an orally active Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator with anticonvulsive properties. ICA 110381 is a KCNQ2/Q3 activator (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.80%
- No. CAS: 325457-99-6
- Fòrmula: C12H8Cl2N2O
- Peso molecular:267.11
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
KV7.1 0.38 μM (EC50) |
KV7.3 0.38 μM (EC50) |
KV7.1 15 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.38 μM
Compound: 16
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Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
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[PMID: 24900334] |
| CHO | IC50 |
15 μM
Compound: 16
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Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
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[PMID: 24900334] |
In Vitro
ICA 110381 induces rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing KCNQ2 or KCNQ3 (EC50 = 0.38 µM). ICA 110381 inhibits rubidium efflux from CHO cells expressing KCNQ1 (EC50 = 15 µM)[1].
In CA1 pyramidal cells, the increase of M-currents (IM) in the presence of ICA 110381 resulted in a damping of neuronal excitability by reducing the input resistance and shifting the resting membrane potential in hyperpolarizing direction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Wistar rats (200-300 g)[2]
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Dosage:3 mg/kg, 10 mg/kg and 30 mg/kg (suspended in 0.5% Hydroxyethyl Cellulose (HY-B2221B))
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Administration:Oral administration; once
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Result:Showed anticonvulsive properties in fully amygdala-kindled rats.
Chemical Information
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No. CAS 325457-99-6
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Appearance Solid
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Peso molecular 267.11
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Fòrmula C12H8Cl2N2O
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Color White to off-white
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SMILES
O=C(NC1=CC=C(Cl)N=C1)C2=CC=C(Cl)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (467.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Amato G, et al. N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy. ACS Med Chem Lett. 2011 Mar 31;2(6):481-4. [Content Brief]
[2]. A Boehlen, et al. The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)-benzamid displays anticonvulsant potential. Br J Pharmacol. 2013 Mar;168(5):1182-200. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7438 mL | 18.7189 mL | 37.4378 mL | 93.5944 mL |
| 5 mM | 0.7488 mL | 3.7438 mL | 7.4876 mL | 18.7189 mL | |
| 10 mM | 0.3744 mL | 1.8719 mL | 3.7438 mL | 9.3594 mL | |
| 15 mM | 0.2496 mL | 1.2479 mL | 2.4959 mL | 6.2396 mL | |
| 20 mM | 0.1872 mL | 0.9359 mL | 1.8719 mL | 4.6797 mL | |
| 25 mM | 0.1498 mL | 0.7488 mL | 1.4975 mL | 3.7438 mL | |
| 30 mM | 0.1248 mL | 0.6240 mL | 1.2479 mL | 3.1198 mL | |
| 40 mM | 0.0936 mL | 0.4680 mL | 0.9359 mL | 2.3399 mL | |
| 50 mM | 0.0749 mL | 0.3744 mL | 0.7488 mL | 1.8719 mL | |
| 60 mM | 0.0624 mL | 0.3120 mL | 0.6240 mL | 1.5599 mL | |
| 80 mM | 0.0468 mL | 0.2340 mL | 0.4680 mL | 1.1699 mL | |
| 100 mM | 0.0374 mL | 0.1872 mL | 0.3744 mL | 0.9359 mL |
ICA 110381 Related Classifications
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