Bardoxolone-methyl-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEBardoxolonemethylCat.No.:HY-13324CASNo.:218600-53-4分?式:C??H??NO?分?量:505.69作?靶點(diǎn):Keap1-Nrf2;Autophagy;Apoptosis;Ferroptosis作?通路:NF-κB;Autophagy;Apoptosis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:25mg/mL(49.44mM;Needultrasonic)掃描?維碼，H2O:<0.1mg/mL(insoluble)運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9775mL9.8875mL19.7750mL5mM0.3955mL1.9775mL3.9550mL10mM0.1977mL0.9887mL1.9775mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。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(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(4.94mM);Clearsolution此?案可獲得≥2.5mg/mL(4.94mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(4.94mM);Clearsolution此?案可獲得≥2.5mg/mL(4.94mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。3.以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。請(qǐng)依序添加每種溶劑：5%DMSO40%PEG3005%Tween-8050%salineSolubility:2.5mg/mL(4.94mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Bardoxolonemethyl(NSC713200;RTA402;CDDOMethylester)?種合成的三萜類化合物，具有潛在的抗腫瘤和抗炎活性，作為Nrf2通路的激活劑和NF-κB途徑的抑制劑。IC50&TargetNrf2[1]體內(nèi)研究Bardoxolonemethyl(30mg/kg,p.o.)decreasesrenalexpressionofmegalinbutnotcubilin,increasescreatinineclearanceandurinaryalbumin-to-creatinineratios,andinducesNrf2cytoprotectivetargetsincynomolgusmonkeys[1].BardoxolonemethylinducesoverallfavorableeffectsontheheartviaitsimprovementineGFRinbothanimalmodelsandclinicaltrials[2].PROTOCOLAnimalTwoseparatein-lifestudiesareconductedincynomolgusmonkeys.Inonestudy,cynomolgusmonkeysAdministration[1](n=9/gender/dosegroup)areadministeredamorphousbardoxolonemethylbyoralgavage,usingsesameoilasthevehicle,at5,30,and300mg/kgoncedailyfor12monthsinaGLPenvironment.Observationsformorbidity,mortality,injury,andtheavailabilityoffoodandwaterareconductedtwicedailyforallanimals.Clinicalobservationsandbodyweightsareconductedandrecordedweekly.Weightdataareanalyzedbycalculatingtheareaundertheweightversustimecurveusingthelineartrapezoidalmethod.Bloodsamplesforclinicalchemistryevaluationsarecollectedfromallanimalspretestandfromallanimalspriortointerim(6-month)andterminal(12-month)necropsies.Anadditionalgroupofmonkeysforeachdosegroupareallowedtorecoverfor4weeks.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2019Oct25;10(1):4878.?EurJMedChem.2020,113030.?JCellSci.2021Mar23;jcs.255273.?MolNeurobiol.2020Aug;57(8):3616-3631.?ToxicolLett.2016Sep30;259:52-59.Seemorecustomervalidationsonwww.MedChemE2/3www.MedChemEwww.MedChemEREFERENCES[1].ReismanSA,etal.BardoxoloneMethylDecreasesMegalinandActivatesNrf2intheKidney.JAmSocNephrol.2012Aug2.[2].McCulloughPA,etal.Cardiacandrenalfunctioninpatientswithtype2diabeteswhohavechronickidneydisease:potentialeffectsofbardoxolonemethyl.DrugDesDevelTher.2012;6:141-9.McePdfHeight關(guān)注MCE中國公眾號(hào)，

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