BiologicalActivity
Potent,ATP-competitiveROCKinhibitor(IC50valuesare52,57and122nMforhumanROCK2,ratROCK2andhumanROCK1respectivelybyELISA);alsoinhibitsPKAC-αandPRKX(IC50valuesare200and325nMrespectively).Exhibitsanalgesiceffectsinratmodelsofinflammatory(AIA)andnoninflammatory(MIA)arthriticpain.Orallybioavailable.
CompoundLibraries
AS1892802isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 333.38 |
| Formula | C20H19N3O2 |
| Storage | StoreatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 928320-12-1 |
| PubChemID | 46911016 |
| InChIKey | WDTFYYZHMRBVHK-LJQANCHMSA-N |
| Smiles | O=C(N[C@H](CO)C3=CC=CC=C3)NC(C=C2)=CC=C2C1=CC=NC=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.34 | 100 | |
| ethanol | 8.33 | 25 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight333.38.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 3mL | 15mL | 30mL |
| 5mM | 0.6mL | 3mL | 6mL |
| 10mM | 0.3mL | 1.5mL | 3mL |
| 50mM | 0.06mL | 0.3mL | 0.6mL |
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ProductDatasheets
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