BQ-3020-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBQ-3020Cat.No.:HY-P1016CASNo.:143113-45-5分?式:C??H???N??O??S分?量:2006.32Sequence:Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-TrpSequenceShortening:Ac-Acetyl-LMDKEAVYFAHLDIIW作?靶點(diǎn):EndothelinReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BQ-3020?種內(nèi)?素受體(endothelinreceptor)(ETBreceptor)激動(dòng)劑，取代[125I]ET-1與豬?腦ETB受體結(jié)合，IC50值為0.2nM。BQ-3020引起兔肺動(dòng)脈?管收縮和豬膀胱頸松弛，可?于??管疾病研究。IC50&TargetETB0.2nM(IC50)體外研究BQ-3020(0.01–300nM,7min),producedconcentration-dependentrelaxationsoonPhE-precontractedurothelium-denudedstrips[1].BQ-3020(0.01–200nM,20min)causespotentdose-dependentvasoconstrictionwithEC50valuesof0.57nMinrabbitpulmonaryarteriesbyinhibitingETBreceptors[2]..體內(nèi)研究BQ-3020(3mg/kgfori.h.,singledose)attenuatescancerpainbyapproximately50%upto3hpost-injectioncomparedtoPBS-vehicleandcontralateralinjectionincancerpainmousemodel[3].AnimalModel:Cancerpainmousemodel[3]Dosage:3mg/kgAdministration:Injectedsubcutaneouslyatthesiteofthegreatesttumordevelopment1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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