BiologicalActivity
PotentRhokinase(ROCK)inhibitor(IC50valuesare1.6and4nMforrecombinanthumanROCK1andROCK2respectively).Displaysgreaterthan30-foldselectivityforROCKagainstapanelofserine/threoninekinases.Inducesvasorelaxationinpreconstrictedrataorta(IC50=35nM);lowersbloodpressureinaratmodelofhypertension.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
CompoundLibraries
GSK269962isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 570.6 |
| Formula | C29H30N8O5 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 850664-21-0 |
| PubChemID | 16095342 |
| InChIKey | YOVNFNXUCOWYSG-UHFFFAOYSA-N |
| Smiles | CCN(C(C4=NON=C4N)=N3)C1=C3C=NC(OC2=CC(NC(C5=CC=C(OCCN6CCOCC6)C=C5)=O)=CC=C2)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.06 | 100 | |
| ethanol | 5.71 | 10mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight570.6.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.75mL | 8.76mL | 17.53mL |
| 5mM | 0.35mL | 1.75mL | 3.51mL |
| 10mM | 0.18mL | 0.88mL | 1.75mL |
| 50mM | 0.04mL | 0.18mL | 0.35mL |
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ProductDatasheets
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