BiologicalActivity
HighaffinityandselectivenegativemodulatorofAMPAreceptorscontainingTARP-γ8(Ki=26nM).Exhibits<50%bindingagainstapanelof52receptors,ionchannelsandtransporters(except5HT2Bandmelatoninreceptors78%and57%,respectively).AlsodisplaysminimalactivityagainstotherTARP-lessAMPARsandAMPARscoexpressedwithotherTARPsorCNIH2.Orallybioavailableandbrainpenetrant.Anticonvulsant.
LicensingInformation
SoldwiththepermissionofJanssenPharmaceuticaN.V.
TechnicalData
| M.Wt | 328.67 |
| Formula | C14H8ClF3N2O2 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 2036081-86-2 |
| Smiles | ClC1=CC=CC(OC(F)(F)F)=C1C2=CC=C3NC(NC3=C2)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.87 | 100 | |
| ethanol | 32.87 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight328.67.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 3.04mL | 15.21mL | 30.43mL |
| 5mM | 0.61mL | 3.04mL | 6.09mL |
| 10mM | 0.3mL | 1.52mL | 3.04mL |
| 50mM | 0.06mL | 0.3mL | 0.61mL |
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