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Selurampanel

Cat. No. M30874
Selurampanel Structure
Synonym:

BGG 492

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 377.42
Formula C16H19N5O4S
CAS Number 912574-69-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Samia Elkommos, et al. Expert Opin Pharmacother. Current and future pharmacotherapy options for drug-resistant epilepsy

[2] Klaus Kucher, et al. Prog Brain Res. Efficacy and safety of single- and repeated-selurampanel dosing for 2 weeks in patients with chronic subjective tinnitus: Results of a randomized, double-blind, placebo-controlled, cross-over, proof-of-concept phase IIa study

[3] Marco Mula. Expert Opin Emerg Drugs. Emerging drugs for focal epilepsy

[4] David Orain, et al. ChemMedChem. Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

[5] Edward Faught. Expert Opin Investig Drugs. BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy

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