Orallyactive,potenthistamineH1antagonist(IC50=4nM)thatdisplays20-fold,>250-foldand>250-foldselectivityover5-HT,dopamineandmuscarinicacetylcholinereceptorsrespectively.Exhibitsantimalarialactivityinmultidrugresistantstrainsinvitro(IC50=227-734nM).AlsopotentKV11.1(hERG)channelblocker(IC50=0.9nM)thatdisplayscardiotoxicityinvivo.
AstemizoleisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
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.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.86 | 100 | |
ethanol | 11.46 | 25 |
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 |