Traceamine1(TA1)receptorantagonist/inverseagonist;exhibitsahigherpotencyatthemouseTA1receptorthantheratandhumanTA1receptors(IC50valuesare27.5,4539and7487nM,respectively).BlockstheTA1receptor-mediatedactivationofaninwardlyrectifyingK+current,whichincreasesthefiringfrequencyofdopamine(DA)neuronsintheventraltegmentalarea.IncreasesDApotencyattheD2receptor.Alsodisplaysinverseagonism,reducingbasalcAMPlevelsinvitro(IC50=19nM).
EPPTBisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
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.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 37.84 | 100 | |
ethanol | 37.84 | 100 |
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 |