Voclosporin-ISAtx-247-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVoclosporinCat.No.:HY-106638CASNo.:515814-01-4Synonyms:ISAtx-247分⼦式:C₆₃H₁₁₁N₁₁O₁₂分⼦量:1214.62作⽤靶点:MolecularGlues;Phosphatase作⽤通路:PROTAC;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(41.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM0.8233mL4.1165mL8.2330mL5mM0.1647mL0.8233mL1.6466mL10mM0.0823mL0.4117mL0.8233mL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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.06mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Voclosporin(ISAtx-247)⼀种钙调神经磷酸酶(CN;PP2B)抑制剂[1]。IC50&TargetCalcineurin[1]体外研究Thisnovelsemi-syntheticcalcineurin(CN)inhibitorisdesignatedVoclosporin(ISATX247).TheefficacyofVoclosporinasanimmunosuppressiveagentisexaminedusinganinvitrocalcineurinassay[1].Voclosporin(ISATX247)isacalcineurininhibitorthathasshownmorepotencythanCyclosporineinvitro[2].体内研究AllanimalstolerateVoclosporin(ISATX247)andCyclosporineA(CsA)verywell.Therearenosevereadverseeffectsassociatedwitheitherdrug.IntheVoclosporingroup,allanimalsexcept1havediarrheaofdifferentdurationsduringthestudy(mean2.3days,range2to7days).ThisdiffersfromtheCsAandthecontrolgroups,wherenoanimalshavediarrhea.MeanweightlossattheendofthestudyisslightlyhigherintheVoclosporingroupthanintheCsAandcontrolgroups(3.4%vs2.0%and1.0%,respectively)[2].PROTOCOLAnimalMonkey[2]Administration[2]Wild-caught,malecynomolgusmonkeys,weighingbetween5and8kg,areused.Fourgroupsofanimalsaretreatedtwicedailyat8:00AMand6:00PMfor7dayswiththefollowingdoses:GroupI(n=6),Voclosporin25mg/kg;GroupII(n=6),Voclosporin50mg/kg;GroupIII(n=5),CsA25mg/kg;andGroupIV(n=4),vehicle(nodrug)1mL/kg.LevelsofCyclosporineandVoclosporininwholebloodaremeasuredbyliquidchromatography/massspectrometry[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AbelMD,etal.ISATX247:anovelcalcineurininhibitor.JHeartLungTransplant.2001Feb;20(2):161.[2].StalderM,etal.InvivoevaluationofthenovelcalcineurininhibitorISATX247innon-humanprimates.JHeartLungTransplant.2003Dec;22(12):1343-52.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical