Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJTE-013Cat.No.:HY-100675CASNo.:383150-41-2分?式:C??H??Cl?N?O分?量:408.29作?靶點(diǎn):LPLReceptor;Apoptosis作?通路:GPCR/GProtein;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(244.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4492mL12.2462mL24.4924mL5mM0.4898mL2.4492mL4.8985mL10mM0.2449mL1.2246mL2.4492mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.83mg/mL(2.03mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.83mg/mL(2.03mM);ClearsolutionBIOLOGICALACTIVITY?物活性JTE-013?種有效且選擇性的S1P2(鞘氨醇1-磷酸2)拮抗劑。JTE-013抑制放射性標(biāo)記的S1P與?和??S1P2的特異性結(jié)合，IC50分別為17nM和22nM。IC50&TargetIC50:17nM(S1P2forhuman)and22nM(S1P2forrat)[1]體外研究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.體內(nèi)研究JTE-013(gavage;30mg/kgdailyfor14consecutivedays)reducestumorsizeandtumorweight[1].AnimalModel:Six-week-oldfemaleathymicNCr-nu/nunudemice[1]Dosage:30mg/kgAdministration:Gavage;dailyfor14consecutivedaysResult:Reducedtumorsizeandtumorweight.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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