BiologicalActivity
ApotentGABAuptakeinhibitor,selectiveforGAT-1(IC50valuesare0.13,550,944and7210μMforhGAT-1,rGAT-2,hGAT-3andhBGT-1respectively).Inhibitstransportcurrentcompetitively(Ki=7μM)andtransmitter-gatedcurrentnon-competitively(Ki=0.03nM).Abletopasstheblood-brainbarrieraftersystemicadmiNISTrationandisactiveinvivo.
LicensingInformation
SoldwiththepermissionofGlaxoSmithKline
CompoundLibraries
SKF89976AhydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
M.Wt | 371.91 |
Formula | C22H25NO2.HCl |
Storage | Desiccateat+4°C |
Purity | ≥99%(HPLC) |
CASNumber | 85375-15-1 |
PubChemID | 6917797 |
InChIKey | SNGGBKYQZVAQKA-UHFFFAOYSA-N |
Smiles | Cl[H].OC(=O)C1CCCN(CCC=C(C2=CC=CC=C2)C2=CC=CC=C2)C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 37.19 | 100 | |
water | 100mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight371.91.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 2.69mL | 13.44mL | 26.89mL |
5mM | 0.54mL | 2.69mL | 5.38mL |
10mM | 0.27mL | 1.34mL | 2.69mL |
50mM | 0.05mL | 0.27mL | 0.54mL |