ASP-4058-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEASP-4058Cat.No.:HY-111021CASNo.:952565-91-2分?式:C??H??F?N?O?分?量:442.31作?靶點(diǎn):LPLReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥50mg/mL(113.04mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2609mL11.3043mL22.6086mL5mM0.4522mL2.2609mL4.5217mL10mM0.2261mL1.1304mL2.2609mL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(protectfromlight)。-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?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(2.83mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:1.25mg/mL(2.83mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.83mM);ClearsolutionBIOLOGICALACTIVITY?物活性ASP-4058?個(gè)選擇性的、?服活性的鞘氨醇磷酸受體1和5(S1P1andS1P5)的?代激動(dòng)劑，能改??實(shí)驗(yàn)性??免疫性腦脊髓炎，具有良好的安全性[1]。IC50&TargetS1P1andS1P5[1].體內(nèi)研究ASP4058(p.o.,dailyfor21days)reducestheclinicalscoreinadose-dependentmannerandthecumulativeclinicalscorefromday0to21dpiat0.03,0.1and0.3mg/kgare15.5±1.48,9.50±2.17and1.17±1.17,respectively,whilethatofvehicle-treatedgroupis15.5±0.619inrats.ASP4058preventsdecreasesinbodyweightofEAErats[1].ASP4058(p.o.,dailyforday12today45)maintainstheclinicalscoreatarelativelylowlevelandthecumulativeclinicalscores(18-45dpi)amongthegroupstreatedwith0.1and0.3mg/kgdosagesare6.90±2.85and5.60±2.21,respectivelyinmice.TheED50valuesforASP4058is0.063mg/kg[1].AnimalModel:MaleLewisratswithaninductionofEAE[1].Dosage:0.03,0.1or0.3mg/kg.Administration:Oraladministrationoncedailyfor21days.Result:Reducedtheclinicalscoreinadose-dependentmannerandthecumulativeclinicalscore.AnimalModel:SJLmiceimmunizedwithPLP139-151andboostedwithpertussistoxindevelopedrelapsing-remittingEAE[1].Dosage:0.1and0.3mg/kgAdministration:Oraladministrationoncedailyfromday12today45.Result:Maintainedtheclinicalscoreatarelativelylowlevelandthecumulativeclinicalscores(18-45dpi).戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SciAdv.2020May29;6(22):eaay8627.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].RieYamamoto,etal.ASP4058,aNovelAgonistforSphingosine1-PhosphateReceptors1and5,AmelioratesRodentExperimentalAutoimmuneEncephalomyelitiswithaFavorableSafetyProfile.PLoSOne.2014Oct27;9(10):e110819.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo