SGC707-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESGC707Cat.No.:HY-19715CASNo.:1687736-54-4分⼦式:C₁₆H₁₈N₄O₂分⼦量:298.34作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(335.19mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3519mL16.7594mL33.5188mL5mM0.6704mL3.3519mL6.7038mL10mM0.3352mL1.6759mL3.3519mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥3mg/mL(10.06mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥3mg/mL(10.06mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥3mg/mL(10.06mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SGC707⼀种强效的、选择性和⾮竞争性的PRMT3(蛋⽩精氨酸甲转移酶3)抑制剂(IC50=31nM,Kd=53nM)。IC50&TargetPRMT331nM(IC50)体外研究SGC707(0-10μM;6h)bindstoPRMT3inbothHEK293andA549cells[1].CellViabilityAssay[1]CellLine:HEK293andA549cellsConcentration:0-10μMIncubationTime:6hoursResult:StabilizedPRMT3inbothHEK293andA549cellswithEC50valuesof1.3μMand1.6μM,respectively.体内研究SGC707(intraperitonealinjection;10mg/kg;3timesperweek;3w)treatmentreduceshepaticsteatosisandplasmatriglyceridelevelsandinducespruritusinWestern-typediet-fedLDLreceptorknockoutmice[2].AnimalModel:Western-typediet-fedLDL(lipoprotein)receptorknockoutmice[2]Dosage:10mg/kgAdministration:Intraperitonealinjection;10mg/kg;3timesperweek;3weeksResult:Exhibited50%lowerlivertriglyceridestoresaswellas32%lowerplasmatriglyceridelevels.户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2019Feb19;116(8):2961-2966.•CellDeathDis.2021Nov9;12(11):1066.•ClinTranslMed.2022Jan;12(1):e686.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•FASEBJ.2020Aug;34(8):10212-10227.•UniversityofMunich.FakultätfürMedizin.2022Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].deJongLM,etal.PRMT3inhibitorSGC707reducestriglyceridelevelsandinducespruritusinWestern-typediet-fedLDLreceptorknockoutmice.SciRep.2022Jan10;12(1):483.[2].KaniskanHÜ,etal.Apotent,selectiveandcell-activeallostericinhibitorofproteinargininemethyltransferase3(PRMT3).AngewChemIntEdEngl.2015Apr20;54(17):5166-70.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical