Lanifibranor-IVA337-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELanifibranorCat.No.:HY-104049CASNo.:927961-18-0Synonyms:IVA337分?式:C??H??ClN?O?S?分?量:434.92作?靶點:PPAR作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(229.93mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2993mL11.4964mL22.9927mL5mM0.4599mL2.2993mL4.5985mL10mM0.2299mL1.1496mL2.2993mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.75mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.78mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.78mM);ClearsolutionBIOLOGICALACTIVITY?物活性Lanifibranor?種泛過氧化物酶體增殖物激活受體(PPAR)的激動劑，對?類PPARα，PPARσ和PPARγ的EC50值分別為1.5,0.87和0.21μM。IC50&TargetPPARγPPARδPPARα206nM(EC50,HumanPPARγ)866nM(EC50,HumanPPAR1537nM(EC50,HumanPPARδ)α)體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemEDec;75(12):2175-2183.McePdfHeightCaution:Producthasnotbeenfullyvalidate