Pirfenidone-AMR69-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPirfenidoneCat.No.:HY-B0673CASNo.:53179-13-8Synonyms:AMR69分?式:C??H??NO分?量:185.22作?靶點(diǎn):TGF-beta/Smad;CCR作?通路:StemCell/Wnt;TGF-beta/Smad;GPCR/GProtein;Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(539.90mM)H2O:16.67mg/mL(90.00mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM5.3990mL26.9949mL53.9898mL5mM1.0798mL5.3990mL10.7980mL10mM0.5399mL2.6995mL5.3990mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：0.5%CMC-Na/salinewaterSolubility:20mg/mL(107.98mM);Clearsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(11.23mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(11.23mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(11.23mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(14.85mM);Clearsolution6.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(14.85mM);Clearsolution7.請(qǐng)依序添加每種溶劑：PBSSolubility:9.09mg/mL(49.08mM);Clearsolution;Needultrasonicandwarmingandheatto60°C8.請(qǐng)依序添加每種溶劑：SalineSolubility:6.67mg/mL(36.01mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Pirfenidone(AMR69)?種抗纖維化劑，可減弱纖維細(xì)胞中CCL2和CCL12的產(chǎn)?。Pirfenidone具有抑制細(xì)胞?長(zhǎng)的作?，并能降低?膠質(zhì)瘤細(xì)胞系中的TGF-β2蛋??平。Pirfenidone還具有抗炎活性。IC50&TargetTGF-β2[1]體外研究Pirfenidone(PFD)reducestheproteinlevelsofthematrixmetalloproteinase(MMP)-11,aTGF-βtargetgeneandfurinsubstrateinvolvedincarcinogenesis.ThesedatadefinePFDorPFD-relatedagentsaspromisingagentsforhumancancersassociatedwithenhancedTGF-βactivity[1].InRAW264.7cells,amurinemacrophage-likecellline,PirfenidonesuppressestheproinflammatorycytokineTNF-αbyatranslationalmechanism,whichisindependentofactivationoftheMAPK2,p38MAPK,andJNK.Inthemurineendotoxinshockmodel,Pirfenidonepotentlyinhibitstheproductionoftheproinflammatorycytokines,TNF-α,interferon-γ,andinterleukin-6,butenhancestheproductionoftheanti-inflammatorycytokine,interleukin-10[2].Pirfenidone(PFD)showsitsinhibitoryeffectsontheproliferationofHLECs.Cellproliferationisattenuatedinthe0.3mg/mLgroupafter24hourscomparewiththecontrolgroup(P=0.044).Theeffectismoreapparentinthe0.5mg/mLgroupat24,48,and72hours(P[3].體內(nèi)研究AdministrationofPirfenidone(300mg/kg/day)for4wk.PirfenidonesignificantlyattenuatesthescorewhenadministeredinBleomycin(BLM)-treatedmice(P[4].PROTOCOL2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellAssay[3]HLECsareseededin96-wellplates(1×104cells/well)for24hoursinα-MEM/10%FBS/1%NEAA,andareculturedinstationarytubesinserum-freemediumfor24hours.Andthentheculturemediumisremovedandcellsarebathedinα-MEMwith10%FBSand1%NEAAsupplementedwith0,0.01,0.1,0.2,0.3,0.5,or1mg/mLPirfenidonefor0,4,12,24,48,or72hours.Afterincubationwith180μLα-MEMand20μLof5mg/mLMTTfor4hoursat37°C,theMTTsolutionisdiscarded.TheFormosanprecipitatesaredissolvedin180μLDMSObyagitatingthedishesfor10minutesat200rpmonanorbitalshaker.Theabsorbanceat490nmineachwellisreadwithamicroplatereader.WefurtherexaminedtheeffectsofPFDbyrefiningtheconcentrationsat0.2,0.25,0.3,0.4,0.5and0.6mg/mLusingtheMTTassay[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[4]Administration[4]Nine-week-oldfemaleC57BL/6miceareused.Pirfenidoneisadministeredorallyfor14daysafterosmoticpumpimplantation.Thevolumeofadministrationisdeterminedaccordingtobodyweight.Animalsareallocatedinto4groups(n=6/group):normalcontrol,BLM,Pirfenidone(300mg/kg/day),andBLM+Pirfenidone.ThePirfenidonedoseisselectedaccordingtoareportpublishedelsewhere.Pirfenidoneisalsoadministeredinatherapeuticsettingbeginningatday10toassesstheeffectofthedrugonthefibroticphaseofBLMmodelmice.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ArthritisRheumatol.2022Sep3.?SciAdv.2022Jun17;8(24):eabn4564.?JExpClinCancerRes.2021Feb9;40(1):62.?CellDeathDis.2022Jul30;13(7):663.?JCIInsight.2021Nov30;e141108.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BurghardtI,etal.PirfenidoneinhibitsTGF-betaexpressioninmalignantgliomacells.BiochemBiophysResCommun.2007Mar9;354(2):542-7.[2].NakazatoH,etal.Anovelanti-fibroticagentpirfenidonesuppressestumornecrosisfactor-alphaatthetranslationallevel.EurJPharmacol.2002Jun20;446(1-3):177-85.[3].YangY,etal.InhibitionofPirfenidoneonTGF-beta2inducedproliferation,migrationandepithlial-mesenchymaltransitionofhumanlensepithelialcellslineSRA01/04.PLoSOne.2013;8(2):e56837.[