DSM265-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDSM265Cat.No.:HY-100184CASNo.:1282041-94-4分⼦式:C₁₄H₁₂F₇N₅S分⼦量:415.33作⽤靶点:DihydroorotateDehydrogenase;Parasite作⽤通路:MetabolicEnzyme/Protease;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(120.39mM;Needultrasonic)Ethanol:11.11mg/mL(26.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4077mL12.0386mL24.0772mL5mM0.4815mL2.4077mL4.8154mL10mM0.2408mL1.2039mL2.4077mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.75mg/mL(6.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(6.62mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DSM265⼀种长效的恶性疟原⾍⼆氢乳酸脱氢酶PfDHODH抑制剂，其IC50值为8.9nM。DSM265还可以抑制Pf3D7的⽣长，其EC50值为4.3nM。IC50&TargetIC50:8.9nM(PfDHODH)[1]EC50:4.3nM(P.falciparum3D7parasites)[1]体内研究DSM265(0.5to75mg/kg;Oraladministration;twicedaily;for4days;NOD-scidIL-2Rγnull(NSG)mice)haspotentinvivoantimalarialactivitywith90%effectivedose(ED90)of3mg/kgperday(1.5mg/kgtwicedaily).Themaximumrateofparasitekillingoccurredatandaboveadoseof13mg/kgperday(6.4mg/kgtwicedaily).DSM265hasmoderateterminaleliminationhalf-life(t1/2)of2-4hoursformice(0.5to75mg/kg,oral)[2].AnimalModel:NOD-scidIL-2Rγnull(NSG)mice(23-36g)[2]Dosage:0.5to75mg/kgAdministration:Oraladministration;twicedaily;for4daysResult:Hadpotentantimalarialactivitywith90%effectivedose(ED90)of3mg/kgperday(1.5mg/kgtwicedaily).REFERENCES[1].KokkondaS,etal.Tetrahydro-2-naphthyland2-IndanylTriazolopyrimidinesTargetingPlasmodiumfalciparumDihydroorotateDehydrogenaseDisplayPotentandSelectiveAntimalarialActivity.JMedChem.2016Jun9;59(11):5416-31.[2].PhillipsMA,etal.Along-durationdihydroorotatedehydrogenaseinhibitor(DSM265)forpreventionandtreatmentofmalaria.SciTranslMed.2015Jul15;7(296):296ra111.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For