1-Aminobenzotriazole-ABT-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE1-AminobenzotriazoleCat.No.:HY-103389CASNo.:1614-12-6Synonyms:ABT;3-Aminobenzotriazole分⼦式:C₆H₆N₄分⼦量:134.14作⽤靶点:CytochromeP450作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(745.49mM;Needultrasonic)H2O:50mg/mL(372.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM7.4549mL37.2745mL74.5490mL5mM1.4910mL7.4549mL14.9098mL10mM0.7455mL3.7274mL7.4549mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(15.51mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(15.51mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(15.51mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:25mg/mL(186.37mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性1-Aminobenzotriazole细胞⾊素P450(P450)的⾮特异且不可逆抑制剂。IC50&TargetP450[1]体外研究1-Aminobenzotriazole(ABT)alonesignificantlyincreasestheexpressionlevelsofCYP2B6intwodifferenthepatocytes(7.3-and10.8-fold,respectively).Uponco-treatmentwith1-Aminobenzotriazole,theinductionofCYP2B6expressionbyCITCOorrifampinispotentiated:12.6-and4.0-foldforCITCOaswellas3.9-and2.5-foldforrifampin.1-AminobenzotriazolehasagreaterpotentiationeffectonCITCOthanonrifampin.1-AminobenzotriazolealoneincreasestheexpressionlevelsofCYP3A4intowdifferenthepatocytes(by2.0-and3.8-fold).Uponco-treatmentwith1-Aminobenzotriazole,theeffectsofCITCOonCYP3A4expressionlevelsarepotentiatedby3.8-and6.0-foldascomparetocellstreatedwithCITCOalone[1].1-Aminobenzotriazole(ABT)(1mM)showspronounced(~95%)inhibitionoftheformationofN-acetylprocainamidecomparewiththecontrolwithout1-Aminobenzotriazole[2].体内研究Oral1-Aminobenzotriazole(ABT)(100mg/kg,2hpredose)decreasestheclearanceofintravenousprocainamide(45%)inrats,accompaniedbyadecreasedN-acetylprocainamide-to-procainamideratioinurine(0.74versus0.21)andplasma(areaunderthecurveratio0.59versus0.11).Theurinaryrecoveryofprocainamideincreasesfrom18to30%,whereastherecoveryofN-acetylprocainamideinurinedecreasesfrom13.3to6.5%with1-Aminobenzotriazole[2].Pretreatmentofratswith100mg/kgoral1-Aminobenzotriazole(ABT)administered2hoursbeforeasemisolidcalorictestmealmarkedlydelaysgastricemptying.1-Aminobenzotriazolealsoincreasesstomachweightsby2-fold[3].PROTOCOLCellAssay[1]Freshlyisolatedhumanhepatocytesareusedinthisstudy.Briefly,hepatocytesareplacedinserum-freeWilliams’Emediacontaining0.1μMdexamethasone,10μg/mLgentamicin,15mMHEPES,2mML-glutamine,and1%ITS.Cellsareincubatedfor10hrat37°Cinanatmospherecontaining5%CO2.Afterrecovery,thehepatocytesaretreatedwithmediacontainingCITCO(100nM),rifampin(10μM)orvehicle(ethanol),withorwithout1-Aminobenzotriazole(ABT)(1mM)for72hr[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalMaleSprague-Dawleyrats(0.26to0.30kg,n=3pertreatment)receiveanoraldoseof1-AminobenzotriazoleAdministration[2](ABT)(100mg/kg,2mL/kg)2hbeforeasingleintravenousbolusofprocainamide(10mg/kg,2mL/kg).Thecontrolgroupreceivesonlytheintravenousbolusofprocainamidewithout1-Aminobenzotriazolepretreatment.Thevehicleforboth1-Aminobenzotriazoleandprocainamideis10%dimethylacetamide/90%water(v/v).Ratsarefed4hafterdosing,andserialbloodsamplesarecollectedat0.03,0.17,0.25,0.5,1,2,4,and6hpostdose.BloodsamplesarecentrifugedusingtubescontainingK3-EDTAastheanticoagulanttoobtainplasma.Urinesamplesarealsocollectedover24hpostdose.Plasmaandurinesamplesarefrozenat-20°Cuntilanalysis[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2021Sep20;12(1):5548.•FrontPharmacol.2022May16;13:848957.•Xenobiotica.2022Oct12;1-47.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YangK,etal.InductionofCYP2B6andCYP3A4expressionby1-aminobenzotriazole(ABT)inhumanhepatocytes.DrugMetabLett.2010Aug;4(3):129-33.[2].SunQ,etal.1-Aminobenzotriazole,aknowncytochromeP450inhibitor,isasubstrateandinhibitorofN-acetyltransferase.DrugMetabDispos.2011Sep;39(9):1674-9.[3].StringerRA,etal.1-AminobenzotriazolemodulatesoraldrugpharmacokineticsthroughcytochromeP450inhibitionanddelayofgastricemptyi