Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECiprofloxacinmonohydrochlorideCat.No.:HY-B0356ACASNo.:93107-08-5Synonyms:Bay-09867monohydrochloride分?式:C??H??ClFN?O?分?量:367.8作?靶點(diǎn):Topoisomerase;Apoptosis;Antibiotic;Bacterial;MitochondrialMetabolism;ReactiveOxygenSpecies作?通路:CellCycle/DNADamage;Apoptosis;Anti-infection;MetabolicEnzyme/Protease;Immunology/Inflammation;NF-κB儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:12.5mg/mL(33.99mM;Needultrasonic)DMSO:5mg/mL(13.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7189mL13.5943mL27.1887mL5mM0.5438mL2.7189mL5.4377mL10mM0.2719mL1.3594mL2.7189mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.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%DMSO>>90%(20%SBE-β-CDinsaline)1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.5mg/mL(1.36mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.5mg/mL(1.36mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ciprofloxacin(Bay-09867)monohydrochloride?種?服有效的拓?fù)洚悩?gòu)酶IV抑制劑。Ciprofloxacinmonohydrochloride誘導(dǎo)線粒體DNA和核DNA損傷并導(dǎo)致線粒體功能障礙和活性氧產(chǎn)?。Ciprofloxacinmonohydrochloride具有抗增殖活性并誘導(dǎo)細(xì)胞凋亡(apoptosis)。Ciprofloxacinmonohydrochloride?種氟喹諾酮類抗?素，具有強(qiáng)?的抗活性。IC50&TargetQuinolone體外研究Ciprofloxacin(Bay-09867)monohydrochloride(5-50μg/mL;0-24h;tendoncells)inhibitscellproliferationandcausescellcyclearrestattheG2/Mphase[1].Ciprofloxacin(Bay-09867)monohydrochlorideshowspotentactivityagainstY.pestisandB.anthraciswithMIC90of0.03μg/mLand0.12μg/mL,respectively[2].CellViabilityAssay[1]CellLine:TendoncellsConcentration:5,10,20and50μg/mLIncubationTime:24hoursResult:Decreasedthecellularityoftendoncells.CellCycleAnalysis[1]CellLine:TendoncellsConcentration:50μg/mLIncubationTime:24hoursResult:ArrestedcellcycleattheG2/Mphaseandinhibitedcelldivisionintendoncells.WesternBlotAnalysis[1]CellLine:TendoncellsConcentration:50μg/mLIncubationTime:0,6,12,17and24hoursResult:Down-regulatedtheexpressionofCDK-1andcyclinBproteinandmRNA.Up-regulated2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEtheexpressionofPLK-1protein.體內(nèi)研究Ciprofloxacin(Bay-09867)monohydrochloride(30mg/kg;i.p.;for24hours;BALB/cmice)hasprotectionagainstY.pestisinmurinemodelofpneumonicplague[3].Ciprofloxacin(Bay-09867)monohydrochloride(100mg/kg;i.g.;daily,for4weeks;C57BL/6Jmice)acceleratesaorticrootenlargementandincreasestheincidenceofaorticdissectionandrupturebydecreasesLOXlevelandincreasesMMPlevelsandactivityintheaorticwall[4].Ciprofloxacin(Bay-09867)monohydrochloride(100mg/kg;i.g.;daily,for4weeks;C57BL/6Jmice)inducesDNAdamageandreleaseofDNAtothecytosol,mitochondrialdysfunction,andactivationofcytosolicDNAsensorsignaling.Ciprofloxacinlactateincreasesapoptosisandnecroptosisintheaorticwall[4].AnimalModel:BALB/cmice[3]Dosage:30mg/kgAdministration:Intraperitonealinjection;for24hoursResult:Reducedthelungbacterialloadinmurinemodelofpneumonicplague.AnimalModel:C57BL/6Jmice[4]Dosage:100mg/kgAdministration:Oralgavage;daily,for4weeksResult:HadaorticdestructionthatwasaccompaniedbydecreasedLOXexpressionandincreasedMMPexpressionandactivity.AnimalModel:C57BL/6Jmice[4]Dosage:100mg/kgAdministration:Oralgavage;daily,for4weeksResult:CausedmitochondrialDNAandnuclearDNAdamage,leadingtomitochondrialdysfunctionandROSproduction.Increasedapoptosisandnecroptosisintheaorticwall.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2022Mar2;13(1):1116.?AdvSci(Weinh).2020Jul21;7(17):2001374.?IntJAntimicrobAgents.2018Aug;52(2):269-271.?EBioMedicine.2022Apr;78:103943.?MicrobiolSpectr.2022Apr25:e0251821.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].TsaiWC,et,al.Ciprofloxacin-mediatedcellproliferationinhibitionandG2/Mcellcyclearrestinrattendoncells.ArthritisRheum.2008Jun;58(6):1657-63.[2].SteenbergenJ,et,al.InVitroandInVivoActivityofOmadacyclineagainstTwoBiothreatPathogens,BacillusanthracisandYersiniapestis.AntimicrobAgentsChemother.2017Apr24;61(5):e02434-16.[3].HamblinKA,et,al.InhaledLiposomalCiprofloxacinProtectsagainstaLethalInfectioninaMurineModelofPneumonicPlague.FrontMicrobiol.2017Feb6;8:91.[4].LeMaireSA,et,al.EffectofCiprofloxacinonSusceptibilitytoAorticDissectionandRuptureinMice.J