1-Aminobenzotriazole-ABT-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE1-AminobenzotriazoleCat.No.:HY-103389CASNo.:1614-12-6Synonyms:ABT;3-Aminobenzotriazole分?式:C?H?N?分?量:134.14作?靶點(diǎn):CytochromeP450作?通路:MetabolicEnzyme/Protease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(745.49mM;Needultrasonic)H2O:50mg/mL(372.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM7.4549mL37.2745mL74.5490mL5mM1.4910mL7.4549mL14.9098mL10mM0.7455mL3.7274mL7.4549mL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)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(15.51mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(15.51mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(15.51mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:25mg/mL(186.37mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性1-Aminobenzotriazole細(xì)胞?素P450(P450)的?特異且不可逆抑制劑。IC50&TargetP450[1]體外研究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].體內(nèi)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?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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