JTE-013-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJTE-013Cat.No.:HY-100675CASNo.:383150-41-2分⼦式:C₁₇H₁₉Cl₂N₇O分⼦量:408.29作⽤靶点:LPLReceptor;Apoptosis作⽤通路:GPCR/GProtein;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(244.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4492mL12.2462mL24.4924mL5mM0.4898mL2.4492mL4.8985mL10mM0.2449mL1.2246mL2.4492mL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%salineSolubility:≥0.83mg/mL(2.03mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.83mg/mL(2.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JTE-013⼀种有效且选择性的S1P2(鞘氨醇1-磷酸2)拮抗剂。JTE-013抑制放射性标记的S1P与⼈和⼤⿏S1P2的特异性结合，IC50分别为17nM和22nM。IC50&TargetIC50:17nM(S1P2forhuman)and22nM(S1P2forrat)[1]体外研究JTE-013(50-200μM;1-3days)reducedcellviability[1].JTE-013(10-1000nM;30mins)reversesS1P-inducedAktinhibitionandinhibitsS1P-inducedERKactivation[1].JTE-013displays4.2%inhibitionofS1P3anddoesnotantagonizeS1P1atconcentrationsupto10μM[1].CellViabilityAssay[1]CellLine:SK-N-AScellsConcentration:50,100,150,200μMIncubationTime:1-3daysResult:Reducedcellviability.WesternBlotAnalysis[1]CellLine:SK-N-AScellsConcentration:10,100,1000nMIncubationTime:30minsResult:ReversedS1P-inducedAktinhibitionandinhibitedS1P-inducedERKactivation.体内研究JTE-013(gavage;30mg/kgdailyfor14consecutivedays)reducestumorsizeandtumorweight[1].AnimalModel:Six-week-oldfemaleathymicNCr-nu/nunudemice[1]Dosage:30mg/kgAdministration:Gavage;dailyfor14consecutivedaysResult:Reducedtumorsizeandtumorweight.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•ExpTherMed.2018Jun;15(6):5007-5016.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiMH,etal.AntitumorActivityofaNovelSphingosine-1-Phosphate2Antagonist,AB1,inNeuroblastoma.JPharmacolExpTher.2015Sep;354(3):261-8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For