BiologicalActivity
GABAAreceptorinverseagonistselectivefortheα5-subtype(EC50=3nM).ExhibitsaffinityatbenzodiazepinebindingsiteofrecombinanthumanGABAAreceptors(Kivaluesare0.77nM,0.83nM,0.85nMand1.4nMforα3-,α1-,α2-,andα5-containingrespectively).Increaseslong-termpotentiation(LTP)inmousehippocampalslices.Exhibitsnoanxiogenicorproconvulsantactivity.
LicensingInformation
ManufacturedandsoldunderlicensefromMerck&Co.,Inc.forusesolelyforpreclinicalresearchpurposes(ie:notforadministrationtoorotheruseinhumans)
CompoundLibraries
MRK016isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 368.39 |
| Formula | C17H20N8O2 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 342652-67-9 |
| PubChemID | 6918583 |
| InChIKey | QYSYOGCIDRANAR-UHFFFAOYSA-N |
| Smiles | CC(C)(C)C2=C1C=NN=C(C4=NOC(C)=C4)N1N=C2OCC3=NC=NN3C |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.84 | 100 | |
| ethanol | 3.68 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight368.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.71mL | 13.57mL | 27.15mL |
| 5mM | 0.54mL | 2.71mL | 5.43mL |
| 10mM | 0.27mL | 1.36mL | 2.71mL |
| 50mM | 0.05mL | 0.27mL | 0.54mL |
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ProductDatasheets
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