BiologicalActivity
Orallyactive,potenthistamineH1antagonist(IC50=4nM)thatdisplays20-fold,>250-foldand>250-foldselectivityover5-HT,dopamineandmuscarinicacetylcholinereceptorsrespectively.Exhibitsantimalarialactivityinmultidrugresistantstrainsinvitro(IC50=227-734nM).AlsopotentKV11.1(hERG)channelblocker(IC50=0.9nM)thatdisplayscardiotoxicityinvivo.
CompoundLibraries
AstemizoleisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 458.57 |
| Formula | C28H31FN4O |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 68844-77-9 |
| PubChemID | 2247 |
| InChIKey | GXDALQBWZGODGZ-UHFFFAOYSA-N |
| Smiles | FC(C=C5)=CC=C5CN2C1=CC=CC=C1N=C2NC3CCN(CCC4=CC=C(OC)C=C4)CC3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.86 | 100 | |
| ethanol | 11.46 | 25 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight458.57.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.18mL | 10.9mL | 21.81mL |
| 5mM | 0.44mL | 2.18mL | 4.36mL |
| 10mM | 0.22mL | 1.09mL | 2.18mL |
| 50mM | 0.04mL | 0.22mL | 0.44mL |
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