Etonogestrel-3-Oxodesogestrel-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEtonogestrelCat.No.:HY-B0652CASNo.:54048-10-1Synonyms:3-Oxodesogestrel;3-keto-Desogestrel分⼦式:C₂₂H₂₈O₂分⼦量:324.46作⽤靶点:EstrogenReceptor/ERR;ProgesteroneReceptor;EndogenousMetabolite;FKBP作⽤通路:Others;MetabolicEnzyme/Protease;Apoptosis;Autophagy;Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(154.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0820mL15.4102mL30.8204mL5mM0.6164mL3.0820mL6.1641mL10mM0.3082mL1.5410mL3.0820mL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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Etonogestrel(3-Oxodesogestrel)孕激素去氧孕烯的⽣物活性代谢物，Etonogestrel与靶器官中的孕酮受体(progesteronereceptor)和雌激素受体(estrogenreceptors)⾼亲和⼒地结合[1]。Etonogestrel诱导FKBP51mRNA和蛋⽩表达[2]。IC50&TargetHumanEndogenousMetabolite体外研究Etonogestrelinhibitsfertilitybyinhibitingthereleaseofluteinizinghormone(LH),oneofthereproductivehormonesimportantinovulation[1].Etonogestrelalsoincreasestheviscosityofcervicalmucus,whichhindersthepassageofspermatozoaandalterstheliningoftheuterustopreventimplantationofafertilizedeggintotheendometrium[1].Etonogestrel,aprogestin,isasubstrateoftheCYP3A4oxidasesystem[1].EtonogestrelinduceFKBP51mRNAandproteinexpressioninculturedhumanendometrialstromalcells(HESCs)[2].WesternBlotAnalysis[2]CellLine:Humanendometrialstromalcells(HESCs)Concentration:100nMIncubationTime:24hoursResult:IncreasedFKBP51mRNAandproteinlevels.REFERENCES[1].http://www.drugbank.ca/drugs/DB00294[2].DionneD.Maddox,etal.Etonogestrel(Implanon),AnotherTreatmentOptionforContraception.PT.2008Jun;33(6):337–347.[3].OzlemGuzelogluKayisli,etal.ProgestinsUpregulateFKBP51ExpressioninHumanEndometrialStromalCellstoInduceFunctionalProgesteroneandGlucocorticoidWithdrawal:ImplicationsforContraceptive-AssociatedAbnormalUterineBleeding.PLoSOne.2015Oct5;10(10):e0137855.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F