Tranilast-MK-341-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETranilastCat.No.:HY-B0195CASNo.:53902-12-8Synonyms:MK-341;SB252218分⼦式:C₁₈H₁₇NO₅分⼦量:327.33作⽤靶点:AngiotensinReceptor;ProstaglandinReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(152.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0550mL15.2751mL30.5502mL5mM0.6110mL3.0550mL6.1100mL10mM0.3055mL1.5275mL3.0550mL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：1.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:4mg/mL(12.22mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.64mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.64mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.64mM);Clearsolution5.请依序添加每种溶剂：30%SBE-β-CDSolubility:5mg/mL(15.28mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Tranilast(MK-341)⼀种抗变态反应剂。抑制前列腺素D2产⽣(PGD2，IC50=0.1mM)。具有抗炎和免疫调节作⽤[1]。Tranilastsodium拮抗⾎管紧张素II(angiotensinII)并抑制其在⾎管平滑肌细胞中的⽣物学作⽤[2]。IC50&TargetAngiotensinII体外研究TranilastexhibitssignificantimmunomodulatoryactivityinhibitingEndotoxin-inducedprostaglandinE2(PGE2;IC50=~1-20μM),thromboxaneB2(IC50=~10-50μM),(TGF-β1;IC50=~100-200μM),andIL-8(IC50=~100μM)formation.A23187-inducedmonocyteleukotrieneC4orPGE2formationisinhibitedbyTranilastatIC50sof10-40μMand2-20μM,respectively[3].Tranilast(10-200μM)exhibitstheanti-proliferativeeffectinadose-dependentmannerinbothMCF-7andMDA-MB-231celllines.Tranilastalso(10-200μM)enhancestheanti-tumoreffectsofTamoxifen(1-20μM)onhumanbreastcancercellsinvitro[4].Tranilast(12.5,25,50,100μg/mL;72hours)inhibitsproliferationofHDMECs[5].CellProliferationAssay[4]CellLine:MCF-7andMDA-MB-231cellsConcentration:10,20,50,100,and200μMIncubationTime:48hoursResult:Anti-proliferativeeffectinadose-dependentmannerinbothcelllines.CellViabilityAssay[5]CellLine:Humandermalmicrovascularendothelialcells(HDMECs)Concentration:12.5,25,50,100μg/mLIncubationTime:72hoursResult:IC50valuewas44.3μg/mL(136μM).2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Tranilast(300mg/kg;administeredorallytwiceadayfor3days)dose-dependentlysuppressesangiogenesisinmice[5].AnimalModel:Nine-week-oldmaleC57BL/6mice[5]Dosage:300mg/kgAdministration:Administeredorallytwiceadayfor3daysResult:SuppressedtheVEGF-inducedangiogenesisinmatrigel;58%ofsignificantsuppressionwasobservedatadoseof300mg/kg.TheED50valueand95%confidencelimitswere165mg/kgand162±169mg/kg,respectively.户使⽤本产品发表的科研⽂献•CellMetab.2022Feb7;34(3):424-440.e7.•Autophagy.2021Nov;17(11):3592-3606.•PharmacolRes.2017Nov;125(PtB):150-160.•JInterferonCytokineRes.2021Mar;41(3):102-110.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KIkai,etal.InhibitoryEffectofTranilastonProstaglandinDSynthetase.BiochemPharmacol.1989Aug15;38(16):2673-6.[2].SaraDarakhshan,etal.TranilastEnhancestheAnti-TumorEffectsofTamoxifenonHumanBreastCancerCellsinVitro.JBiomedSci.2013Oct21;20(1):76.[3].EACapper,etal.ModulationofHumanMonocyteActivitiesbyTranilast,SB252218,aCompoundDemonstratingEfficacyinRestenosis.JPharmacolExpTher.2000Dec;295(3):1061-9.[4].MIsaji,etal.TranilastInhibitstheProliferation,ChemotaxisandTubeFormationofHumanMicrovascularEndothelialCellsinVitroandAngiogenesisinVivo.BrJPharmacol.1997Nov;122(6):1061-6.[5].KMiyazawa,etal.TranilastAntagonizesAngiotensinIIandInhibitsItsBiologicalEffectsinVascularSmoothMuscleCells.Atherosclerosis.1996Apr5;121(2):