BAY-549-ROCK-IN-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBAY-549Cat.No.:HY-10319CASNo.:867017-68-3Synonyms:ROCK-IN-2;Azaindole1;TC-S7001分?式:C??H??ClF?N?O分?量:402.79作?靶點:ROCK作?通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:33.33mg/mL(82.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4827mL12.4134mL24.8268mL5mM0.4965mL2.4827mL4.9654mL10mM0.2483mL1.2413mL2.4827mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.21mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.21mM);ClearsolutionBIOLOGICALACTIVITY?物活性BAY-549(Azaindole1)有?服活性，ATP-競爭型的ROCK抑制劑，對ROCK-1和ROCK-2的IC50值分別為0.6和1.1nM。IC50&TargetROCK-1ROCK-2TRKFLT30.6nM(IC50)1.1nM(IC50)252nM(IC50)303nM(IC50)體外研究BAY-549(Azaindole1)isahighlypotentinhibitorofhumanROCK-1andROCK-2,withIC50sof0.6and1.1?nM,respectively,andalsoinhibitsmurineROCK-2orratROCK-2withIC50sof2.4and0.8?nM,respectively.BAY-549alsoinhibitsreceptortyrosinekinasesTRKandFLT3,withIC50sof252and303?nM,respectively,butshowsslightinhibitionofMLCKandZIP-kinasewithIC50sof7.4?μMand4.1?μM,respectively.BAY-549inducesvasorelaxationinvitro,andsuppressesthephenylephrine-inducedcontractionofrabbitsaphenousarteryinaconcentrationdependentmannerwithanIC50valueof65?nM[1].體內(nèi)研究BAY-549(Azaindole1)(0.03,0.1,0.3?mg/kg,i.v.)resultsinadose-dependentandlong-lastingdecreaseinbloodpressureinanaesthetizednormotensiverats.BAY-549(3and10?mg/kg,p.o.)decreasesbloodpressuredose-dependentlyandpersistentlybothinnormotensiveandhypertensiverats,andshowssucheffectsevenat1?mg/kginhypertensiverats.BAY-549(0.1and0.3?mg/kg,i.v.bolusinjections)causesdecreasedmeanarterialbloodpressureinadose-relatedmannerandonlyleadstoamoderateanddose-independentincreaseinheartrateofanaesthetizeddogs[1].PROTOCOLAnimalMaleWistarratsweighing300-350?gareanaesthetizedwiththiopental100?mg/kgintraperitoneally(i.p.).AAdministration[1]tracheotomyisperformedandcathetersareinsertedintothefemoralarteryforbloodpressureandheartratemeasurementsandintothefemoralveinfortestdrugadministration.Theanimalsareventilatedwithroomairandtheirbodytemperatureiscontrolled.ROCK-IN-2isadministeredintravenously(i.v.)indosesof0.03-0.1?mg/kg.ThevehicleTranscutol/CremophorEL/physiologicalsaline(19/10/80=v/v/v)withouttestdrugisusedascontrol.Thevolumeadministeredis1?mL/kg.Sixanimalsaretreatedpergroup[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MolTher-NuclAcids.2021May28.?JCIInsight.2018Jun7;3(11).pii:98921.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].KastR,etal.Cardiovasculareffectsofanovelpotentandhighlyselectiveazaindole-basedinhibitorofRho-kinase.BrJPharmacol.2007Dec;152(7):1070-80.Epub2007Oct15.McePdfHeightCaution:Produ