Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETranilastCat.No.:HY-B0195CASNo.:53902-12-8Synonyms:MK-341;SB252218分?式:C??H??NO?分?量:327.33作?靶點(diǎn):AngiotensinReceptor;ProstaglandinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(152.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0550mL15.2751mL30.5502mL5mM0.6110mL3.0550mL6.1100mL10mM0.3055mL1.5275mL3.0550mL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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(shí)驗(yàn)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：1.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:4mg/mL(12.22mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.64mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.64mM);Suspendedsolution;Needultrasonic4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.64mM);Clearsolution5.請依序添加每種溶劑：30%SBE-β-CDSolubility:5mg/mL(15.28mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Tranilast(MK-341)?種抗變態(tài)反應(yīng)劑。抑制前列腺素D2產(chǎn)?(PGD2，IC50=0.1mM)。具有抗炎和免疫調(diào)節(jié)作?[1]。Tranilastsodium拮抗?管緊張素II(angiotensinII)并抑制其在?管平滑肌細(xì)胞中的?物學(xué)作?[2]。IC50&TargetAngiotensinII體外研究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?邊的抑制劑?師www.MedChemE體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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):