Sarecycline-P-005672-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemESarecyclineCat.No.:HY-16770CASNo.:1035654-66-0Synonyms:P-005672分子式:C₂₄H₂₉N₃O₈分子量:487.5作用靶点:Antibiotic;Bacterial;DNA/RNASynthesis作用通路:Anti-infection;CellCycle/DNADamage储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:100mg/mL(205.13mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制备储备液1mM2.0513mL10.2564mL20.5128mL5mM0.4103mL2.0513mL4.1026mL10mM0.2051mL1.0256mL2.0513mL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方式配制澄清的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄清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是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)请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.13mM);Clearsolution请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.13mM);ClearsolutionBIOLOGICALACTIVITY1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE生物活性Sarecycline是一种口服有效的窄谱四环素衍生物类抗生素。Sarecycline具有抗炎活性。Sarecycline能够抑制革兰氏阳性细菌和多种痤疮角质杆菌的活性。Sarecycline干扰tRNA调节并将mRNA与70S核糖体结合。Sarecycline能够用于中重度痤疮的研究[1][2][3][4][5][6]。体外研究Sarecyclineinhibits55clinicalisolatesofC.acnes,andtheMICvaluesforSarecyclinerangedfrom0.5to16µg/ml;theMIC50was0.5µg/ml,andtheMIC90was4 µg/ml[1].Sarecyclineexhibitsactivityagainstthemacrolide-resistantorganisms[1].SarecyclinehydrochlorideexhibitsminimalactivityagainstentericaerobicGram-negativebacteria[2].体内研究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.客户使用本产品发表的科研文献Pharmaceutics.2021,13(12),2085.MicrobiolSpectr.2023May4;e0071823.MicrobiolSpectr.2022Dec8;e0323822.ClinExpPharmacolPhysiol.2023Apr22.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3 MasterofBioactiveMolecules—您身边的抑制剂大师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