| Identification | Back Directory | [Name]
N-(6-Chloropyridin-3-Yl)-3,4-Difluorobenzamide | [CAS]
325457-89-4 | [Synonyms]
ICA-027243
N-(6-Chloropyridin-3-Yl)-3,4-Difluorobenzamide
Benzamide, N-(6-chloro-3-pyridinyl)-3,4-difluoro-
antiepileptic,hyperpolarization,ICA-27243,opener,Inhibitor,KcsA,Potassium Channel,inhibit,KCNQ3,KCNQ2,ICA 27243,anticonvulsant,ICA27243 | [Molecular Formula]
C12H7ClF2N2O | [MDL Number]
MFCD17166959 | [MOL File]
325457-89-4.mol | [Molecular Weight]
268.65 |
| Chemical Properties | Back Directory | [Boiling point ]
318.5±42.0 °C(Predicted) | [density ]
1.476±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Sparingly Soluble: 1-10 mg/ml | [form ]
Solid | [pka]
10.40±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects[1][2]. | [in vivo]
ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED50 of 8.4 mg/kg) in the mouse maximal electroshock epilepsy model[1]. | Animal Model: | Male CD-1 mice with electroshock assay[1] | | Dosage: | 1-100 mg/kg | | Administration: | Oral administration | | Result: | Produced a dose-dependent increase in the latency to hind limb extension, exhibiting an ED50 value of 8.4 mg/kg.
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| [References]
[1] Wickenden AD, et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. Mol Pharmacol. 2008 Mar;73(3):977-86. DOI:10.1124/mol.107.043216
[2] 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. DOI:10.1021/ml200053x |
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