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Potent,ATP-competitiveROCKinhibitor(IC50valuesare52,57and122nMforhumanROCK2,ratROCK2andhumanROCK1respectivelybyELISA);alsoinhibitsPKAC-αandPRKX(IC50valuesare200and325nMrespectively).Exhibitsanalgesiceffectsinratmodelsofinflammatory(AIA)andnoninflammatory(MIA)arthriticpain.Orallybioavailable.
AS1892802isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight333.38.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Lietal(2012)Fragment-basedandstructure-guideddiscoveryandoptimizationofRhokinaseinhibitors.J.Med.Chem.552474PMID:22272748
Yoshimietal(2010)AntinociceptiveeffectsofAS1892802,anovelRhokinaseinhibitor,inratmodelsofinflammatoryandnoninflammatoryarthritis.J.Pharmacol.Exp.Ther.334955PMID:20534789
Keywords:AS1892802,supplier,AS1892802,rho,kinases,ROCK1,ROCK2,potent,selective,inhibitors,inhibits,ATP,competitive,pain,analgesics,analgesia,chronic,arthritis,antiinflammatory,MIA,AIA,orally,bioavailable,Rho-kinases,Rho-kinases,TocrisBioscience
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