BAY-549-ROCK-IN-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY-549Cat.No.:HY-10319CASNo.:867017-68-3Synonyms:ROCK-IN-2;Azaindole1;TC-S7001分⼦式:C₁₈H₁₃ClF₂N₆O分⼦量:402.79作⽤靶点:ROCK作⽤通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(82.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4827mL12.4134mL24.8268mL5mM0.4965mL2.4827mL4.9654mL10mM0.2483mL1.2413mL2.4827mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.21mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.21mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BAY-549(Azaindole1)有⼝服活性，ATP-竞争型的ROCK抑制剂，对ROCK-1和ROCK-2的IC50值分别为0.6和1.1nM。IC50&TargetROCK-1ROCK-2TRKFLT30.6nM(IC50)1.1nM(IC50)252nM(IC50)303nM(IC50)体外研究BAY-549(Azaindole1)isahighlypotentinhibitorofhumanROCK-1andROCK-2,withIC50sof0.6and1.1ꢀnM,respectively,andalsoinhibitsmurineROCK-2orratROCK-2withIC50sof2.4and0.8ꢀnM,respectively.BAY-549alsoinhibitsreceptortyrosinekinasesTRKandFLT3,withIC50sof252and303ꢀnM,respectively,butshowsslightinhibitionofMLCKandZIP-kinasewithIC50sof7.4ꢀμMand4.1ꢀμM,respectively.BAY-549inducesvasorelaxationinvitro,andsuppressesthephenylephrine-inducedcontractionofrabbitsaphenousarteryinaconcentrationdependentmannerwithanIC50valueof65ꢀnM[1].体内研究BAY-549(Azaindole1)(0.03,0.1,0.3ꢀmg/kg,i.v.)resultsinadose-dependentandlong-lastingdecreaseinbloodpressureinanaesthetizednormotensiverats.BAY-549(3and10ꢀmg/kg,p.o.)decreasesbloodpressuredose-dependentlyandpersistentlybothinnormotensiveandhypertensiverats,andshowssucheffectsevenat1ꢀmg/kginhypertensiverats.BAY-549(0.1and0.3ꢀmg/kg,i.v.bolusinjections)causesdecreasedmeanarterialbloodpressureinadose-relatedmannerandonlyleadstoamoderateanddose-independentincreaseinheartrateofanaesthetizeddogs[1].PROTOCOLAnimalMaleWistarratsweighing300-350ꢀgareanaesthetizedwiththiopental100ꢀmg/kgintraperitoneally(i.p.).AAdministration[1]tracheotomyisperformedandcathetersareinsertedintothefemoralarteryforbloodpressureandheartratemeasurementsandintothefemoralveinfortestdrugadministration.Theanimalsareventilatedwithroomairandtheirbodytemperatureiscontrolled.ROCK-IN-2isadministeredintravenously(i.v.)indosesof0.03-0.1ꢀmg/kg.ThevehicleTranscutol/CremophorEL/physiologicalsaline(19/10/80=v/v/v)withouttestdrugisusedascontrol.Thevolumeadministeredis1ꢀmL/kg.Sixanimalsaretreatedpergroup[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•MolTher-NuclAcids.2021May28.•JCIInsight.2018Jun7;3(11).pii:98921.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].KastR,etal.Cardiovasculareffectsofanovelpotentandhighlyselectiveazaindole-basedinhibitorofRho-kinase.BrJPharmacol.2007Dec;152(7):1070-80.Epub2007Oct15.McePdfHeightCaution:Produ