BQ-3020-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBQ-3020Cat.No.:HY-P1016CASNo.:143113-45-5分⼦式:C₉₆H₁₄₀N₂₀O₂₅S分⼦量:2006.32Sequence:Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-TrpSequenceShortening:Ac-Acetyl-LMDKEAVYFAHLDIIW作⽤靶点:EndothelinReceptor作⽤通路:GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BQ-3020⼀种内⽪素受体(endothelinreceptor)(ETBreceptor)激动剂，取代[125I]ET-1与猪⼩脑ETB受体结合，IC50值为0.2nM。BQ-3020引起兔肺动脉⾎管收缩和猪膀胱颈松弛，可⽤于⼼⾎管疾病研究。IC50&TargetETB0.2nM(IC50)体外研究BQ-3020(0.01–300nM,7min),producedconcentration-dependentrelaxationsoonPhE-precontractedurothelium-denudedstrips[1].BQ-3020(0.01–200nM,20min)causespotentdose-dependentvasoconstrictionwithEC50valuesof0.57nMinrabbitpulmonaryarteriesbyinhibitingETBreceptors[2]..体内研究BQ-3020(3mg/kgfori.h.,singledose)attenuatescancerpainbyapproximately50%upto3hpost-injectioncomparedtoPBS-vehicleandcontralateralinjectionincancerpainmousemodel[3].AnimalModel:Cancerpainmousemodel[3]Dosage:3mg/kgAdministration:Injectedsubcutaneouslyatthesiteofthegreatesttumordevelopment1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Attenuatedcancerpainbyapproximately50%upto3hpost-injectioncomparedtoPBS-vehicleandcontralateralinjectionREFERENCES[1].ArteagaJL,et.al.EndothelinET(B)receptorsareinvolvedintherelaxationtothepigurinarybladderneck.NeurourolUrodyn.2012Jun;31(5):688-94.[2].IharaM,et.al.Anovelradioligand[125I]BQ-3020selectiveforendothelin(ETB)receptors.LifeSci.1992;51(6):PL47-52.[3].QuangPN,et.al.PeripheralendothelinBreceptoragonist-inducedantinociceptioninvolvesendogenousopioidsinmice.Pain.2010May;149(2):254-262.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820