Description
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug. Cenobamate (YKP3089) protects against MES induced seizures in mice with an ED50 of 9.8 mg/kg i.p., and in rats with an ED50 of 1.9 mg/kg p.o. In the sc Met seizures model, Cenobamate given ip inhibited the clonic seizures in mice and rats, with ED50 values of 28.5 and 13.6 mg/kg, respectively. Cenobamate is also effective against seizure induced by picrotoxin with an ED50 of 34.5 mg/kg in mice. Cenobamate is effective in reducing significantly the expression of stage 5 seizures in the hippocampal kindled rat (ED50=16.4 mg/kg). Cenobamate 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 also protects against lithiumpilocarpine-induced intractable seizures in rats (ip) (ED50=7.0 mg/kg). . 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. . 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.
Product information
CAS Number: 913088-80-9
Molecular Weight: 267.67
Formula: C10H10ClN5O2
Chemical Name: (1R)-1-(2-chlorophenyl)-2-(2H-1,2,3,4-tetrazol-2-yl)ethyl carbamate
Smiles: NC(=O)O[C@@H](CN1N=NC=N1)C1=CC=CC=C1Cl
InChiKey: GFHAXPJGXSQLPT-VIFPVBQESA-N
InChi: InChI=1S/C10H10ClN5O2/c11-8-4-2-1-3-7(8)9(18-10(12)17)5-16-14-6-13-15-16/h1-4,6,9H,5H2,(H2,12,17)/t9-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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