W146-TFA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEW146TFACat.No.:HY-101395ACASNo.:909725-62-8分?式:C??H??F?N?O?P分?量:456.39作?靶點(diǎn):LPLReceptor;Apoptosis作?通路:GPCR/GProtein;Apoptosis儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:55mg/mL(120.51mM;ultrasonicandwarmingandheatto60°C)Ethanol:<1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1911mL10.9555mL21.9111mL5mM0.4382mL2.1911mL4.3822mL10mM0.2191mL1.0956mL2.1911mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性W146TFA1-磷酸-鞘氨醇受體亞型1(S1PR1)的選擇性拮抗劑，EC50值為398nM。IC50&TargetEC50:398nM(S1PR1)[1].體外研究W146isaS1PR1antagonistwithaKiof~70-80nM[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEW146pretreatmentsignificantlyincreasesactivatedcleavedcaspase-3levels.ThereducedEPCsapoptosiswhichinducedbyS1PiscompletelyabolishedaftertreatmentwithW146[2].ApoptosisAnalysis[2]CellLine:Endothelialprogenitorcells(EPCs).Concentration:10μM.IncubationTime:30minbeforetheadditionofS1P.Result:Increasesactivatedcleavedcaspase-3levels.體內(nèi)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