Senazodan-hydrochloride-MCI-154-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESenazodanhydrochlorideCat.No.:HY-101693ACASNo.:98326-33-1Synonyms:MCI154hydrochloride分⼦式:C₁₅H₁₅ClN₄O分⼦量:302.76作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:50mg/mL(165.15mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3029mL16.5147mL33.0295mL5mM0.6606mL3.3029mL6.6059mL10mM0.3303mL1.6515mL3.3029mL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(sealedstorage,awayfrommoistureandlight)。-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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.26mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Senazodan(MCI154)(hydrochloride)⼀种Ca2+感光剂，同时可抑制PDEIII的活性。IC50&TargetPDEIII[1]体外研究Senazodan(hydrochloride)seemstoaffectdirectlytheactin-myosincrossbridgekinetics,andincreasesmyosinATPaseactivity[1].Senazodan(hydrochloride)producesaconcentration-dependentincreaseintensiondevelopment.Senazodan(hydrochloride)enhancesCa2+bindingtomyofilamentsandtopurifiedcardiactroponinC.Senazodan(hydrochloride)alsoenhancescontractilityinguinea-pigpapillarymusclesbyinhibitingPDEIII[2].Senazodan(0.1nM~0.1mM)(hydrochloride)showsthatthecontractileresponseofsuperiormesentericarterie(SMA)tonorepinephrine(NE)afterhemorrhagicshockissignificantlydecreasedascomparedwiththenormalcontrolgroup.Senazodan(0.01mM)(hydrochloride)pretreatmentpreventstheeffectsofAngII,andtheconcentration-responsecurveofCa2+isshiftedtotherightascomparedwithAngII-alonegroup[3].体内研究Senazodan(0.1~2.0mg/kg;leftfemoralveincatheterizationinfusion)(hydrochloride)decreasesthepressoreffectofnorepinephrine(NE)[3].Senazodan(0.1mg/kg;i.v.)(hydrochloride)makesLVSP,IP,MC,andLoallincreasedsignificantly,whileheartrateisnotobviouslychangedandleftventricularend-diastolicpressure(LVEDP)isreducedremarkably[4].AnimalModel:Wistarrats(200~250g)[3]Dosage:0.1~2.0mg/kgAdministration:LeftfemoralveincatheterizationinfusionResult:Decreasedthepressoreffectofnorepinephrine(NE).AnimalModel:Rabbits[4]Dosage:0.1mg/kgAdministration:I.v.Result:LVSP,IP,MC,andLoallwereincreasedsignificantlywhileheartratewasnotobviouslychangedandleftventricularend-diastolicpressure(LVEDP)wasreducedremarkably.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].LehtonenLA,etal.Pharmacokineticsandpharmacodynamicsofintravenousinotropicagents.ClinPharmacokinet.2004;43(3):187-203.[2].ErhardtL.Anemergingroleforcalciumsensitisationinthetreatmentofheartfailure.ExpertOpinInvestigDrugs.2005Jun;14(6):659-70.[3].YangG,etal.EffectsofMCI-154onvascularreactivityanditsmechanismsafterhemorrhagicshockinrats.JCardiovascPharmacol.2006;47(6):751-757.[4].MingMJ,etal.EffectsofMCI-154,acalciumsensitizer,oncardiacdysfunctioninendotoxicshockinrabbits.Shock.2000;13(6):459-463.McePdfHeightCaution:Produc