W146-TFA-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEW146TFACat.No.:HY-101395ACASNo.:909725-62-8分⼦式:C₁₈H₂₈F₃N₂O₆P分⼦量:456.39作⽤靶点:LPLReceptor;Apoptosis作⽤通路:GPCR/GProtein;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:55mg/mL(120.51mM;ultrasonicandwarmingandheatto60°C)Ethanol:<1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1911mL10.9555mL21.9111mL5mM0.4382mL2.1911mL4.3822mL10mM0.2191mL1.0956mL2.1911mL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,awayfrommoistureandlight)。-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。BIOLOGICALACTIVITY⽣物活性W146TFA1-磷酸-鞘氨醇受体亚型1(S1PR1)的选择性拮抗剂，EC50值为398nM。IC50&TargetEC50:398nM(S1PR1)[1].体外研究W146isaS1PR1antagonistwithaKiof~70-80nM[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEW146pretreatmentsignificantlyincreasesactivatedcleavedcaspase-3levels.ThereducedEPCsapoptosiswhichinducedbyS1PiscompletelyabolishedaftertreatmentwithW146[2].ApoptosisAnalysis[2]CellLine:Endothelialprogenitorcells(EPCs).Concentration:10μM.IncubationTime:30minbeforetheadditionofS1P.Result:Increasesactivatedcleavedcaspase-3levels.体内研究W146(5mg/kg,ip,priortoAMD3100administration)pre-treatmentshowsapproximately8-foldincreaseofKSL-HSPCmobilization,measuredbytheCFU-G/Mcolonyformingassays,comparedtothatinmicetreatedwithAMD3100alone[3]TheW146-mediatedaugmentationofKSL-HSPCmobilizationisspecific,becausepretreatmentofmicewithW140isunabletoproduceanyeffectonAMD3100-stimulatedKSL-HSPCmobilization.InjectionsofW146,W140,JTE013,orCay10444donotalterthebasalWBCcountinmice[3].AnimalModel:Mice(4-6-week-old)[3].Dosage:5mg/kg.Administration:IP,1hourpriortoAMD3100(ADM)administration.Result:SignificantlyincreasedinKSL-HSPCmobilizationcomparedtothatinmicepretreatedwithdextranfollowedbyAMD3100administration.REFERENCES[1].MGermanaSanna,etal.EnhancementofcapillaryleakageandrestorationoflymphocyteegressbyachiralS1P1antagonistinvivo.NatChemBiol.2006Aug;2(8):434-41.Epub2006Jul9.[2].JingjingLiu,etal.3-amino-4-(3-hexylphenylamino)-4-oxobutylphosphonicacid(W146),aSelectiveAntagonistofSphingosine-1-phospahteReceptorSubtype1,EnhancesAMD3100-stimulatedMobilizationofHematopoieticStemProgenitorCellsinAnimals.JBioc[3].HangWang,etal.Sphingosine-1-phosphatepromotestheproliferationandattenuatesapoptosisofEndothelialprogenitorcellsviaS1PR1/S1PR3/PI3K/Aktpathway.CellBiolInt.2018May23.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic