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Membrane transporter/Ion channel Sodium Channel Cenobamate

Cenobamate

Catalog No. T10757L   CAS 913088-80-9
Synonyms: YKP3089

Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has the potential to be a versatile CNS drug.

Cenobamate, CAS 913088-80-9
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has the potential to be a versatile CNS drug.
Targets&IC50 Sodium channel,   GABA receptor,  
In vivo Cenobamate (YKP3089) is effective in reducing significantly the expression of stage 5 seizures in the hippocampal kindled rat (ED50: 16.4 mg/kg) and it also is effective in the mouse 6 Hz psychomotor seizure model at 22, 32 and 44 mA with ED50 values of 11.0, 17.9 and 16.5 mg/kg, respectively. Cenobamate is also effective against seizure-induced by picrotoxin (ED50: 34.5 mg/kg) in mice. Cenobamate protects against MES induced seizures in mice (ED50: 9.8 mg/kg i.p.) and in rats (ED50: 1.9 mg/kg p.o.) and it also protects against lithium pilocarpine-induced intractable seizures in rats (i.p., ED50: 7.0 mg/kg). Cenobamate given i.p inhibited the clonic seizures in mice and rats (ED50: 28.5 and 13.6 mg/kg), in the sc Met seizures model [2].
Synonyms YKP3089
Purity 98.00%
Molecular Weight 267.67
Formula C10H10ClN5O2
CAS No. 913088-80-9

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 126 mg/mL (470.73 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Zaccara G, et al. Do traditional anti-seizure drugs have a future? A review of potential anti-seizure drugs in clinical development. Pharmacol Res. 2016 Feb;104:38-48. 2. Bialer M, et al. Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.

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