BQ-123-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBQ-123Cat.No.:HY-12378CASNo.:136553-81-6分⼦式:C₃₁H₄₂N₆O₇分⼦量:610.7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:50mg/mL(81.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6375mL8.1873mL16.3747mL5mM0.3275mL1.6375mL3.2749mL10mM0.1637mL0.8187mL1.6375mL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。-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:≥5mg/mL(8.19mM);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:≥5mg/mL(8.19mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(8.19mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BQ-123⼀种⾼效、选择性内⽪素A(ETA)受体拮抗剂，IC50值为7.3nM，Ki值为25nM。BQ-123抑制内⽪素-1介导的⼈肺动脉平滑肌细胞增殖，降低⾼⾎压⼤⿏⾎压。IC50&TargetIC50:7.3nM(EndothelinAreceptors)[1]Ki:25nM(EndothelinAreceptors)[2]体内研究SustainedinfusionsofBQ-123(0.16-164nmol/kgpermin,intravenously,for6h)producesdose-dependentreductionsinmeanarterialpressureinspontaneouslyhypertensiverats(SHR),themaximalreductionbeingobtainedwithadoseof16nmol/kgpermin[4].BQ-123(3mg/kg;i.v.;given15minutesbeforepentylenetetrazole(PTZ))impedestheformationandspreadofseizuretoagreatdegreeinPTZ(50mg/kg;i.p.)+BQ-123groups[5].AnimalModel:MaleWistaralbinorats[5]Dosage:3mg/kgAdministration:Intravenousinjection;given15minutesbeforePTZResult:Numberofratswithmajorseizuredecreased.户使⽤本产品发表的科研⽂献•PLoSPathog.2020Oct19;16(10):e1008947.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].IharaM,etal.Invitrobiologicalprofileofahighlypotentnovelendothelin(ET)antagonistBQ-123selectivefortheETAreceptor.JCardiovascPharmacol.1992;20Suppl12:S11-S14.[2].SakamotoA,etal.DistinctsubdomainsofhumanendothelinreceptorsdeterminetheirselectivitytoendothelinA-selectiveantagonistandendothelinB-selectiveagonists.JBiolChem.1993Apr25;268(12):8547-53.[3].ErdoganHetal.Theprotectiveeffectsofendothelin-AreceptorantagonistBQ-123inpentylenetetrazole-inducedseizureinrats.HumExpToxicol,2014Oct,33(10):1008-16.[4].ZamoraMA,etal.BQ123,anETAreceptorantagonist,inhibitsendothelin-1-mediatedproliferationofhumanpulmonaryarterysmoothmusclecells.AmJRespirCellMolBiol.1993;9(4):429-433.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[5].DouglasSA,etal.BQ-123,aselectiveendothelinsubtypeA-receptorantagonist,lowersbloodpressureindifferentratmodelsofhypertension.JHypertens.1994;12(5):561-567.McePdfHeightCaution:Producthasnotbeenfullyvalidat