Elagolix-sodium-NBI-56418-sodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEElagolixsodiumCat.No.:HY-14369CASNo.:832720-36-2Synonyms:NBI-56418sodium分⼦式:C₃₂H₂₉F₅N₃NaO₅分⼦量:653.57作⽤靶点:GnRHReceptor作⽤通路:GPCR/GProtein储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:50mg/mL(76.50mM;Needultrasonic)H2O:≥50mg/mL(76.50mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5301mL7.6503mL15.3006mL5mM0.3060mL1.5301mL3.0601mL10mM0.1530mL0.7650mL1.5301mL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(sealedstorage,awayfrommoisture)。-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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.83mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.83mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.83mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:130mg/mL(198.91mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Elagolixsodium⼀种⼈的GnRH受体(GnRHR)拮抗剂，其IC50和Ki值分别为0.25和3.7nM。IC50&TargetIC50:0.25nM(GnRHR)[1]Ki:3.7nM(GnRHR)[2]体外研究ElagolixsodiumisahumanGnRHreceptor(GnRHR)antagonistwithanIC50of0.25nMinKinaseassay.Elagolixsodiumhasadvancedtophase3trialsforthetreatmentofendometriosisanduterinefibroids.ElagolixsodiumalsoshowsNFATinhibitionwithanIC50of5.4nMandeffectivelyblocksCa2+fluxwithanIC50of0.86nM[1].KinaseassayalsodemonstratesthatElagolixsodiumisahumanGnRHreceptor(GnRHR)antagonistwithaKivalueof3.7nM[2].PROTOCOLKinaseAssay[2]TheaffinityofElagolixsodiumforhGnRH-RisdeterminedbyacompetitivedisplacementoftheradioligandGnRHfrommembranespreparedfromHEK293cellsstablytransfectedwiththefull-lengthhumanGnRHreceptor[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[2]RBL-1cellsstablyexpressingthehumanclonedGnRHreceptorareseededinto96wellplatesatadensityof15000cellsperwellininositol-freeDMEMcontaining10%dialyzedFBS,10mMHEPES,2mML-glutamine,1mMsodiumpyruvate,0.1mMnonessentialaminoacids,and50μg/mLpenicillin/streptomycinandarelabeledfor48hwith0.2μCimyo-2-[3H]inositol.ThecellsarewashedonceinPBSandpretreatedwithassaybufferfor15to60minat37°C.ThecellsarethenstimulatedwithGnRH(6nM)inthepresenceorabsenceofElagolixsodiumandincubatedfor60minat37°C[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].KimSM,etal.DiscoveryofanOrallyBioavailableGonadotropin-ReleasingHormoneReceptorAntagonist.JMedChem.2016Oct13;59(19):9150-9172.Epub2016Sep27.[2].ChenC,etal.DiscoveryofsodiumR-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate(elagolix),apotentandorallyavailablenonpeptideantagonis2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthas