Nebentan-YM598-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemENebentanCat.No.:HY-106994CASNo.:403604-85-3Synonyms:YM598freebase分?式:C??H??N?O?S分?量:491.52作?靶點:EndothelinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(254.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0345mL10.1725mL20.3451mL5mM0.4069mL2.0345mL4.0690mL10mM0.2035mL1.0173mL2.0345mL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，并請注意儲備液的保存?式和期限。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，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.23mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.23mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Nebentan(YM598freebase)?種有效的具有?服活性的?肽類內(nèi)?素受體(ETAreceptor)拮抗劑，通過Bosentan(HY-A0013)修飾得到。Nebentan抑制[125I]內(nèi)?素-1與?內(nèi)?素ETA和ETB受體結(jié)合，Ki分別為0.697nM和569nM。Nebentan可?于改肺?病和?肌梗死的相關(guān)研究。IC50&TargetETAETB0.697nM(Ki)569nM(Ki)體外研究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].體內(nèi)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