BiologicalActivity
SelectiveRho-kinaseinhibitor(IC50valuesare14,780and1940nMforROCK1,RSKandp70S6Krespectively).Reversesadrenalin-inducedcontractionoftherataorticring(IC50=190nM)andcausesadose-dependentdecreaseinmeanarterialbloodpressureinspontaneoushypertensiverats.Orallyactive.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
CompoundLibraries
GSK429286isalsoofferedaspartoftheTocriscreenPlusandTocriscreenStemCellToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 432.37 |
| Formula | C21H16F4N4O2 |
| Storage | Storeat+4°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 864082-47-3 |
| PubChemID | 11373846 |
| InChIKey | OLIIUAHHAZEXEX-UHFFFAOYSA-N |
| Smiles | O=C1CC(C2=CC=C(C(F)(F)F)C=C2)C(C(NC3=C(F)C=C(NN=C4)C4=C3)=O)=C(C)N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.24 | 100 | |
| ethanol | 10.81 | 25 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight432.37.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.31mL | 11.56mL | 23.13mL |
| 5mM | 0.46mL | 2.31mL | 4.63mL |
| 10mM | 0.23mL | 1.16mL | 2.31mL |
| 50mM | 0.05mL | 0.23mL | 0.46mL |
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