Selurampanel

Research use only, not for human use.

Selurampanel (BGG 492) is a selective, orally active and competitive AMPA receptor (AMPAR) antagonist with IC50 of 0.19 uM.

Selurampanel (BGG 492) is a selective, orally active and competitive AMPA receptor (AMPAR) antagonist with IC50 of 0.19 uM; displays >100-fold selectivity over NMDA and kainate receptors; demonstrates excellent oral potency against MES-induced generalized tonic-clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy.Epilepsy Discontinued.

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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.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.

BGG 492

Membrane Transporter/Ion Channel

iGluR

iGluR

Neurological Disease

Epilepsy

912574-69-7

377.418

C16H19N5O4S

>98% (HPLC)

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CS(=O)(NN1C(NC2=C(C=C(C3=CC=NN3C)C(C(C)C)=C2)C1=O)=O)=O

N-(7-isopropyl-6-(1-methyl-1H-pyrazol-5-yl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)methanesulfonamide

(-20℃)

With Ice Pack

≥ 2 years