Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEG15Cat.No.:HY-103449CASNo.:1161002-05-6分?式:C??H??BrNO?分?量:370.24作?靶點:EstrogenReceptor/ERR作?通路:Others儲存?式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:41.67mg/mL(112.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7010mL13.5048mL27.0095mL5mM0.5402mL2.7010mL5.4019mL10mM0.2701mL1.3505mL2.7010mL請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.62mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.62mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性G15?種?親和?和選擇性G蛋?偶聯(lián)雌激素受體(GPER/GPR30)拮抗劑，Ki值為20nM[1][2]。IC50&TargetKi:20nM(GPER/GPR30)[2]體外研究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.體內研究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.戶使?本產品發(fā)表的科研?獻?EnvironInt.6October2022,107568.?EnvironPollut.2021Jan1;268(PtB):115748.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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