BiologicalActivity
Traceamine1(TA1)receptorantagonist/inverseagonist;exhibitsahigherpotencyatthemouseTA1receptorthantheratandhumanTA1receptors(IC50valuesare27.5,4539and7487nM,respectively).BlockstheTA1receptor-mediatedactivationofaninwardlyrectifyingK+current,whichincreasesthefiringfrequencyofdopamine(DA)neuronsintheventraltegmentalarea.IncreasesDApotencyattheD2receptor.Alsodisplaysinverseagonism,reducingbasalcAMPlevelsinvitro(IC50=19nM).
CompoundLibraries
EPPTBisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 378.39 |
| Formula | C20H21F3N2O2 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 1110781-88-8 |
| PubChemID | 25175634 |
| InChIKey | KLFVWQCQUXXLOU-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC(OCC)=CC=C3)C1=CC(C(F)(F)F)=C(N2CCCC2)C=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.84 | 100 | |
| ethanol | 37.84 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight378.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.64mL | 13.21mL | 26.43mL |
| 5mM | 0.53mL | 2.64mL | 5.29mL |
| 10mM | 0.26mL | 1.32mL | 2.64mL |
| 50mM | 0.05mL | 0.26mL | 0.53mL |
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