Liarozole-R75251-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELiarozoleCat.No.:HY-106019CASNo.:115575-11-6Synonyms:R75251分?式:C??H??ClN?分?量:308.76作?靶點:CytochromeP450;RAR/RXR作?通路:MetabolicEnzyme/Protease儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(323.88mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2388mL16.1938mL32.3876mL5mM0.6478mL3.2388mL6.4775mL10mM0.3239mL1.6194mL3.2388mL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(protectfromlight)。-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%salineSolubility:≥2.5mg/mL(8.10mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.10mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.10mM);ClearsolutionBIOLOGICALACTIVITY?物活性Liarozole(R75251;R85246)?種咪唑衍?物和具有?服活性的維甲酸(RA)代謝阻斷劑(RAMBA)。Liarozole抑制維甲酸依賴的細(xì)胞?素P450(CYP26)4-羥化(IC50=7μM)，導(dǎo)致組織維甲酸?平增加。Liarozole具有抗腫瘤特性[1][2][3]。IC50&TargetCytochromeP450(CYP26)7μM(IC50)體外研究Liarozole(0.01~10μM;9days;MCF-7cells)inhibitscellsproliferation[3].Liarozole(1μM;4days;mesenchymalcells)completelyinhibitschondrogenesis[4].CellProliferationAssay[3]CellLine:MCF-7cellsConcentration:0.01~10μMIncubationTime:9daysResult:Hadaneffectof35%inhibitionat10μMoncellproliferation.CellDifferentiationAssay[4]CellLine:MesenchymalcellsConcentration:1μMIncubationTime:4daysResult:Completelyinhibitedchondrogenesis.體內(nèi)研究Liarozole(5-20mg/kg;p.o.;3days)reversesthevaginalkeratosiscausedbyestrogenstimulation[5].Liarozole(40mg/kg;p.o.;21days)reducestumorburdensubstantially[6].AnimalModel:Ovariectomizedrats[5]Dosage:5~20mg/kgAdministration:P.o.;3days2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Reversedthevaginalkeratosiscausedbyestrogenstimulation.AnimalModel:SCIDmice[6]Dosage:40mg/kgAdministration:P.o.;21daysResult:Inhibitedtumorgrowthandsurvival.REFERENCES[1].KuijpersAL,etal.Theeffectsoforalliarozoleonepidermalproliferationanddifferentiationinsevereplaquepsoriasisarecomparablewiththoseofacitretin.BrJDermatol.1998;139(3):380-389.[2].LuckerGP,etal.OraltreatmentofichthyosisbythecytochromeP-450inhibitorliarozole.BrJDermatol.1997;136(1):71-75.[3].WoutersW,etal.Effectsofliarozole,anewantitumoralcompound,onretinoicacid-inducedinhibitionofcellgrowthandonretinoicacidmetabolisminMCF-7humanbreastcancercells.CancerRes.1992;52(10):2841-2846.[4].PignatelloMA,etal.Liarozolemarkedlyincreasesalltrans-retinoicacidtoxicityinmouselimbbudcellcultures:amodeltoexplainthepotencyofthearomaticretinoid(E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl]benzoicacid.ToxicolApplPharmacol.2002;178(3):186-194.[5].VanWauweJ,etal.Liarozole,aninhibitorofretinoicacidmetabolism,exertsretinoid-mimeticeffectsinvivo.JPharmacolExpTher.1992;261(2):773-779.[6].StearnsME,etal.Liarozoleand13-cis-retinoicacidanti-prostatictumoractivity[publishedcorrectionappearsinCancerRes1993Dec1;53(23):5831].CancerRes.1993;53(13):3073-3077.McePdfHeightCaution:Produ