BiologicalActivity
Selective,orallyactive5-HT6antagonist(pKivaluesare9.02-8.92,6.55,6.35,6.27,6.05,5.95,5.76,5.73,5.62,5.55,5.41,5.39,5.27and<4.99at5-HT6,5-HT1D,5-HT1A,D3,5-HT1B,5-HT1F,α1B,5-HT2C,5-HT2A,D2,5-HT2B,5-HT7,5-HT4and5-HT1Erespectively)andis>200-foldselectiveover55otherreceptors,enzymesandionchannels.Increasesextracellularglutamateandaspartateinthefrontalcortex,andexhibitsanticonvulsantactivity(EC50=0.16μM).
LicensingInformation
SoldwiththepermissionofGlaxoSmithKline
CompoundLibraries
SB271046hydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 488.45 |
| Formula | C20H22ClN3O3S2.HCl |
| Storage | DesiccateatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 209481-24-3 |
| PubChemID | 6918455 |
| InChIKey | RMXZRJYGJMSDQK-UHFFFAOYSA-N |
| Smiles | CC2=C(S(NC3=CC=C(OC)C(N4CCNCC4)=C3)(=O)=O)SC1=CC=C(Cl)C=C12.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.84 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight488.45.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.05mL | 10.24mL | 20.47mL |
| 5mM | 0.41mL | 2.05mL | 4.09mL |
| 10mM | 0.2mL | 1.02mL | 2.05mL |
| 50mM | 0.04mL | 0.2mL | 0.41mL |
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