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Flupirtine maleate

Cat. No. M6735
Flupirtine maleate Structure
Size Price Availability Quantity
10mg USD 53  USD53 In stock
50mg USD 68  USD68 In stock
100mg USD 93  USD93 In stock
500mg USD 355  USD355 In stock
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Quality Control & Documentation
Biological Activity

Flupirtine maleate is a selective potassium channel opener, NMDA receptor antagonist and GABAA receptor modulator. Flupirtine maleate is a non-opioid analgesic with muscle relaxant properties. Activates KV7 potassium channels, indirectly antagonizes NMDA receptors and modulates GABAA receptors. Exhibits neuroprotective actions in a model of cerebral ischemia in mice and reduces apoptosis and necrosis induced by noxious stimuli.

Chemical Information
Molecular Weight 420.4
Formula C15H17FN4O2.C4H4O4
CAS Number 75507-68-5
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage 2-8°C, dry, sealed
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] Din. Curr Opin Investig Drugs. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome.

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