Nebentan-YM598-free-base-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemENebentanCat.No.:HY-106994CASNo.:403604-85-3Synonyms:YM598freebase分⼦式:C₂₄H₂₁N₅O₅S分⼦量:491.52作⽤靶点:EndothelinReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(254.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0345mL10.1725mL20.3451mL5mM0.4069mL2.0345mL4.0690mL10mM0.2035mL1.0173mL2.0345mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.23mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.23mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Nebentan(YM598freebase)⼀种有效的具有⼝服活性的⾮肽类内⽪素受体(ETAreceptor)拮抗剂，通过Bosentan(HY-A0013)修饰得到。Nebentan抑制[125I]内⽪素-1与⼈内⽪素ETA和ETB受体结合，Ki分别为0.697nM和569nM。Nebentan可⽤于改肺⼼病和⼼肌梗死的相关研究。IC50&TargetETAETB0.697nM(Ki)569nM(Ki)体外研究Nebentaninhibitsthespecificbindingof[125I]endothelin-1toendothelinETAandETBreceptorsinaconcentrationdependentmanner,Kivaluesare0.697nMand1.53nMforhumanandratendothelinETAreceptors,respectively.Incontrast,YM598exhibitslowaffinitiesforhumanandratendothelinETBreceptors,withKivaluesof569nMand155nM,respectively[1].InmeasurementofintracellularCa2+concentration,Nebentanconcentration-dependentlyinhibitstheincreasein[Ca2+]iinducedby10nMendothelin-1inbothCHOcellsandA10cells,theIC50valuesare26.2nMforCHOcellsand26.7nMforA10cells,respectively[1].体内研究Nebentan(oraladministration;0.1-1mg/kg;4weeks)significantlyinhibitstheprogressionofpulmonaryhypertensionandthedevelopmentofrightventricularhypertrophy[2].Nebentan(oraladministration;1mg/kg;30weeks)significantlyamelioratesthepoorsurvivalrateofCHFrats,itmarkedlyreducesthehypertrophyofbothventriclesaswellaspulmonarycongestion[2].REFERENCES[1].HironoriYuyama,etal.PharmacologicalCharacterizationofYM598,anOrallyActiveandHighlyPotentSelectiveEndothelinET(A)ReceptorAntagonist.EurJPharmacol.2003Sep30;478(1):61-71.[2].AkiraFujimori,etal.YM598,anOrallyActiveET(A)ReceptorAntagonist,AmelioratestheProgressionofCardiopulmonaryChangesandBoth-SideHeartFailureinRatsWithCorPulmonaleandMyocardialInfarction.JCardiovascPharmacol.2004Nov;44Suppl1:S354-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp