Ascomycin-Immunomycin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAscomycinCat.No.:HY-13557CASNo.:104987-12-4Synonyms:Immunomycin;FR-900520;FK520分⼦式:C₄₃H₆₉NO₁₂分⼦量:792.01作⽤靶点:FKBP;Parasite;Fungal;Antibiotic作⽤通路:Apoptosis;Autophagy;Immunology/Inflammation;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥39mg/mL(49.24mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.2626mL6.3131mL12.6261mL5mM0.2525mL1.2626mL2.5252mL10mM0.1263mL0.6313mL1.2626mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(2.63mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(3.16mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.63mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ascomycin(Immunomycin;FR-900520;FK520)Tacrolimus(FK506)的⼄类似物，具有很强的免疫抑制特性。Ascomycin也⼀种⼤环聚酮类抗⽣素，具有抗疟疾、抗真和抗痉挛等多种⽣物活性。Ascomycin可防⽌移植排斥，并具有⽤于各种⽪肤病研究的潜⼒。IC50&TargetPlasmodium体外研究Ascomycin(FR-900520)suppressesimmuneresponseinvitrowithanIC50valueof0.55nMformousemixedlymphocytereaction[1].Ascomycinisapowerfulcalcium-dependentserine/threonineproteinphosphatase(calcineurin[CaN],proteinphosphatase2B)inhibitors.ItsmechanismofactioninvolvestheformationofamolecularcomplexwiththeintracellularFK506-bindingprotein-12(FKBP12),therebyacquiringtheabilitytointeractwithCaNandtointerferewiththedephosphorylationofvarioussubstrates[3].体内研究Ascomycin(FR-900520;i.m.;0.32-32mg/kg;5daysaweek;for2weeks)clearlyprolongsskinallograftsurvivalinrats[1].AnimalModel:WKArats(8-10weeksold)transplantedwithF344skinallografts[1]Dosage:0.32mg/kg,1mg/kg,3.2mg/kg,10mg/kg,32mg/kgAdministration:i.m.;5daysaweek;for2weeksResult:Clearlyprolongedskinallograftsurvivalinrats户使⽤本产品发表的科研⽂献•ProcNatlAcadSciUSA.2021Jan12;118(2):e2009539118.•MBio.2017Oct24;8(5).pii:e01752-17.•NeurochemRes.2019Feb;44(2):465-471.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HatanakaH,etal.FR-900520andFR-900523,novelimmunosuppressantsisolatedfromaStreptomyces.II.Fermentation,isolationandphysico-chemicalandbiologicalcharacteristics.JAntibiot(Tokyo).1988Nov;41(11):1592-601.[2].KrishikaSambyal,etal.Bioprocessandgeneticengineeringaspectsofascomycinproduction:areview.JGenetEngBiotechnol.2020Nov19;18(1):73.[3].GermánSierra-Paredes,etal.AscomycinandFK506:pharmacologyandtherapeuticpotentialasanticonvulsantsandneuroprotectants.CNSNeurosciTher.Spring2008;14(1):36-46.McePdfHeightCaution:Producthasnotbeenfully