For research use only. Not for therapeutic Use.
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research[1][2].
Selurampanel (Compound 1S) potently and dose-dependently antagonizes maximal electroshock seizure (MES)-induced generalized tonic-clonic seizures in mice with an ED50 value around 7 mg/kg after 1 h pre-treatment[1].
In a study with a 3 mg/kg i.v. dose, a mouse plasma half-life of 3.3 h is determined, with a moderate volume of distribution (Vdss=1.3 L/kg) and a low clearance of 5.4 mL/min▪kg[1].
| Catalog Number | I009429 |
| CAS Number | 912574-69-7 |
| Synonyms | N-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-propan-2-yl-1H-quinazolin-3-yl]methanesulfonamide |
| Molecular Formula | C16H19N5O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C16H19N5O4S/c1-9(2)10-8-13-12(7-11(10)14-5-6-17-20(14)3)15(22)21(16(23)18-13)19-26(4,24)25/h5-9,19H,1-4H3,(H,18,23) |
| InChIKey | MCECSFFXUPEPDB-UHFFFAOYSA-N |
| SMILES | CC(C)C1=C(C=C2C(=C1)NC(=O)N(C2=O)NS(=O)(=O)C)C3=CC=NN3C |
| Reference | [1]. David Orain, et al. Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist. ChemMedChem. 2017 Feb 3;12(3):197-201. [2]. Edward Faught, et al. BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Expert Opin Investig Drugs. 2014 Jan;23(1):107-13. |
