Lanifibranor-IVA337-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELanifibranorCat.No.:HY-104049CASNo.:927961-18-0Synonyms:IVA337分⼦式:C₁₉H₁₅ClN₂O₄S₂分⼦量:434.92作⽤靶点:PPAR作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(229.93mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2993mL11.4964mL22.9927mL5mM0.4599mL2.2993mL4.5985mL10mM0.2299mL1.1496mL2.2993mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.75mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.78mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.78mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Lanifibranor⼀种泛过氧化物酶体增殖物激活受体(PPAR)的激动剂，对⼈类PPARα，PPARσ和PPARγ的EC50值分别为1.5,0.87和0.21μM。IC50&TargetPPARγPPARδPPARα206nM(EC50,HumanPPARγ)866nM(EC50,HumanPPAR1537nM(EC50,HumanPPARδ)α)体内研究Lanifibranorisapanperoxisomeproliferator-activatedreceptor(PPAR)agonistwithEC50sof1.5,0.87and0.21μMforhumanPPARα,PPARσandPPARγ[1].SkinfibrosisisattenuatedbyLanifibranor(IVA337)(p[2].PROTOCOLAnimalMale,aged6weeks,C57BL/6miceareusedindifferentanimaltrials.(i)ExperimentaldermalfibrosisAdministration[2](preventativemodel)isinducedwithbleomycin(n=6eachgroup).Concurrenttreatmentwithlocalinjectionsofbleomycin(0.5mg/mL)andeitherLanifibranor(IVA337)(30mg/kg),Lanifibranor(100mg/kg)orvehiclebydailyoralgavagecontinuedfor3weeks.(ii)Experimentaldermalfibrosis(curativemodel)isinducedusingsubcutaneousbleomycinfor6weeks,but3weeksafterthefirstinjection,micearegivenadailydoseofeitherLanifibranor(30mg/kg),Lanifibranor(100mg/kg)orvehiclebyoralgavagefortheremaining3weeks[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Biomaterials.2022Sep28;290:121817.•Cells.2020Apr14;9(4):964.•CellBiolToxicol.2020Jul1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BoubiaB,etal.Design,Synthesis,andEvaluationofaNovelSeriesofIndoleSulfonamidePeroxisomeProliferatorActivatedReceptor(PPAR)α/γ/δTripleActivators:DiscoveryofLanifibranor,aNewAntifibroticClinicalCandidate.JMedChem.2018Feb27[2].RuzehajiN,etal.PanPPARagonistIVA337iseffectiveinpreventionandtreatmentofexperimentalskinfibrosis.AnnRheumDis.20162/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDec;75(12):2175-2183.McePdfHeightCaution:Producthasnotbeenfullyvalidate