G15-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEG15Cat.No.:HY-103449CASNo.:1161002-05-6分⼦式:C₁₉H₁₆BrNO₂分⼦量:370.24作⽤靶点:EstrogenReceptor/ERR作⽤通路:Others储存⽅式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:41.67mg/mL(112.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7010mL13.5048mL27.0095mL5mM0.5402mL2.7010mL5.4019mL10mM0.2701mL1.3505mL2.7010mL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(protectfromlight)。-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:≥2.08mg/mL(5.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.62mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性G15⼀种⾼亲和⼒和选择性G蛋⽩偶联雌激素受体(GPER/GPR30)拮抗剂，Ki值为20nM[1][2]。IC50&TargetKi:20nM(GPER/GPR30)[2]体外研究G15(0.1-10μM;2days)inhibitsGPER-mediatedproliferationstimulatedby17β-estradiol(E2)inA549andH1793celllines[1].G15(1μM;48hours)inhibitstheresponseofGPERstimulatedbyE2andG1inA549andH1793celllines[1].CellProliferationAssay[1]CellLine:A549,H1793celllinesConcentration:0.1,1,10μM(combinationwith10nME2)IncubationTime:2daysResult:InhibitedGPER-mediatedproliferationstimulatedbyE2.WesternBlotAnalysis[1]CellLine:A549,H1793celllinesConcentration:1μM(combinationwith10nME2and10nMG1)IncubationTime:48hoursResult:InhibitedtheresponseofGPERstimulatedbyE2andG1.体内研究G15(1.46mg/kg;i.h.;twiceaweekfor14weeks)decreasesthenumberoftumornodulesandtumorindexincreasedbytheE2orG1groupinurethane-inducedadenocarcinomamice[1].AnimalModel:Four-week-oldfemaleKunmingmice(Urethane-inducedadenocarcinoma)[1]Dosage:1.46mg/kg(combinationwithE2,0.09mg/kgandfulvestrant(Ful),2.4mg/kg)Administration:Subcutaneousinjection;twiceaweekfor14weeksResult:ThenumberoftumornodulesdecreasedintheE2+Ful+G15group.户使⽤本产品发表的科研⽂献•EnvironInt.6October2022,107568.•EnvironPollut.2021Jan1;268(PtB):115748.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellDeathDis.2022Apr19;13(4):372.•LifeSci.2022May28;120676.•JClinEndocrinolMetab.2021Feb1;dgab020.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiuC,etal.G-Protein-CoupledEstrogenReceptorAntagonistG15DecreasesEstrogen-InducedDevelopmentofNon-SmallCellLungCancer.OncolRes.2019Feb21;27(3):283-292[2].GirgertR,etal.EstrogenSignalinginERα-NegativeBreastCancer:ERβandGPER.FrontEndocrinol(Lausanne).2019Jan9;9:781.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo