Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESarecyclineCat.No.:HY-16770CASNo.:1035654-66-0Synonyms:P-005672分子式:C??H??N?O?分子量:487.5作用靶點:Antibiotic;Bacterial;DNA/RNASynthesis作用通路:Anti-infection;CellCycle/DNADamage儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(205.13mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制備儲備液1mM2.0513mL10.2564mL20.5128mL5mM0.4103mL2.0513mL4.1026mL10mM0.2051mL1.0256mL2.0513mL體內(nèi)實驗請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊埾劝凑誌nVitro方式配制澄清的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶)請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.13mM);Clearsolution請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.13mM);ClearsolutionBIOLOGICALACTIVITY1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE生物活性Sarecycline是一種口服有效的窄譜四環(huán)素衍生物類抗生素。Sarecycline具有抗炎活性。Sarecycline能夠抑制革蘭氏陽性細菌和多種痤瘡角質(zhì)桿菌的活性。Sarecycline干擾tRNA調(diào)節(jié)并將mRNA與70S核糖體結(jié)合。Sarecycline能夠用于中重度痤瘡的研究[1][2][3][4][5][6]。體外研究Sarecyclineinhibits55clinicalisolatesofC.acnes,andtheMICvaluesforSarecyclinerangedfrom0.5to16μg/ml;theMIC50was0.5μg/ml,andtheMIC90was4?μg/ml[1].Sarecyclineexhibitsactivityagainstthemacrolide-resistantorganisms[1].SarecyclinehydrochlorideexhibitsminimalactivityagainstentericaerobicGram-negativebacteria[2].體內(nèi)研究Sarecyclinehydrochloride(0.33-9?mg/kg;i.v.)showpotentactivityagainstS.aureusinamurineneutropenicthighinfectionmodel[1].SarecyclinecaninhibitS.aureus(PD50=0.25mg/kg),buthasnosignificanteffectonE.colievenatthehighestdose(>40mg/kg)inCD-1micemodelofsystemic(intraperitoneal)infection[6].Sarecycline(1-150mg/kg;Intraperitonealinjection;Singledose)showsanti-inflammatoryactivityinSpragueDawleyratsmodel[6].AnimalModel:Carrageenan-inducedfootpadedemamaleSpragueDawleyratsmodel[6]Dosage:1mg/kg,5mg/kg,10mg/kg,25mg/kg,50mg/kg,75mg/kg,100mg/kg,150mg/kgAdministration:Intraperitonealinjection(i.p.);Singledose.Beforeasubplantarinjectionofsterile1mg/0.1mLcarrageenansolutionintherighthindpaw.Result:Reducedinflammationto55.7%and53.1%,respectively,atdosesof75mg/kgand100mg/kgcomparedtobaseline.AnimalModel:Carrageenan-inducedfootpadedemamaleSpragueDawleyratsmodel[6]Dosage:0.33,1,3,or9?mg/kgAdministration:IntravenouslyResult:Achieveda2-log10reductioninthebacterialburdeninthethighatadosecomparabletothatofdoxycycline,withED50sof8.23and8.32?mg/kg,respectively.客戶使用本產(chǎn)品發(fā)表的科研文獻Pharmaceutics.2021,13(12),2085.MicrobiolSpectr.2023May4;e0071823.MicrobiolSpectr.2022Dec8;e0323822.ClinExpPharmacolPhysiol.2023Apr22.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEZhanelG,etal.MicrobiologicalProfileofSarecycline,aNovelTargetedSpectrumTetracyclinefortheTreatmentofAcneVulgaris.AntimicrobAgentsChemother.2018Dec21;63(1):e01297-18.MooreAY,etal.Sarecycline:anarrowspectrumtetracyclineforthetreatmentofmoderate-to-severeacnevulgaris.FutureMicrobiol.2019Sep;14(14):1235-1242.BatoolZ,etal.SarecyclineinterfereswithtRNAaccommodationandtethersmRNAtothe70Sribosome.ProcNatlAcadSciUSA.2020Aug25;117(34):20530-20537.ButlerMS,etal.Antibioticsintheclinicalpipelinein2013.JAntibiot(Tokyo).2013Oct;66(10):571-91.MooreAY,etal.Sarecycline:anarrowspectrumtetracyclineforthetreatmentofmoderate-to-severeacnevulgaris.FutureMicrobiol.2019Sep;14(14):1235-1242.BunickCG,etal.AntibacterialMechanismsandEfficacyofSarecyclineinAnimalModelsofInfectionandInflammation.Antibiotics(Basel).2021Apr15;10(4):439.McePdfHeight