Spectinomycin-dihydrochloride-pentahydrate-Spectinomycin-hydrochloride-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESpectinomycindihydrochloridepentahydrateCat.No.:HY-B1828ACASNo.:22189-32-8Synonyms:Spectinomycinhydrochloridehydrate分?式:C??H??Cl?N?O??分?量:495.35作?靶點(diǎn):Bacterial;Antibiotic作?通路:Anti-infection儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:62.5mg/mL(126.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0188mL10.0939mL20.1877mL5mM0.4038mL2.0188mL4.0375mL10mM0.2019mL1.0094mL2.0188mL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(sealedstorage,awayfrommoisture)。-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.請(qǐng)依序添加每種溶劑：PBSSolubility:50mg/mL(100.94mM);Clearsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Spectinomycindihydrochloridepentahydrate?種?譜抗?素，可以抑制多種?蘭?陽(yáng)性和?蘭?性細(xì)的?長(zhǎng)。Spectinomycindihydrochloridepentahydrate通過(guò)特異靶向細(xì)核糖體，?擾蛋?質(zhì)合成。Spectinomycindihydrochloridepentahydrate也td內(nèi)含?RNA的?競(jìng)爭(zhēng)性抑制劑，Ki為7.2mM。IC50&Targetbacterialribosomalsubunit[5]體外研究SpectinomycindihydrochloridepentahydrateselectivelyinhibitsproteinsynthesisincellsandinextractsofEscherichiacoli:Spectinomycindihydrochloridepentahydrate(50μg/mL)inhibitsEscherichiacoligrowthrapidlyandreversibly,andsuppressesaminoacidincorporationimmediately[1].Spectinomycindihydrochloridepentahydrate(1μg/mLor3μM)inhibitspolypeptidesynthesisdirectedeitherbyendogenousmessengerRNAorbyMS-2bacteriophageRNA,withmaximuminhibitionof70-80%inextractsofEscherichiacoli[1].Spectinomycindihydrochloridepentahydrateblocksthetranslocationofpeptidyl-tRNAsfromA-sitetoP-sitebyinhibitingthebindingofelongationfactorGtotheribosome[2].SpectinomycindihydrochloridepentahydrateinteractsspecificallywiththeresiduesG1064and01192in16SrRNAandpotentiallymakesitinactive[2].SpectinomycindihydrochloridepentahydrateexhibitssplicinginhibitionanddependentonpHchangesandMg2+concentration,indicatingelectrostaticinteractionswiththeintronRNA[3].體內(nèi)研究Spectinomycindihydrochloridepentahydrate(20mg/kg;i.m.;20-100mg/kg;9d)showsthesafetyinhealthychicks[4].Spectinomycindihydrochloridepentahydrate(10mg/kg;i.v.;singledose)hasthemajoreliminationpathwaybyrenalexcretion,approximately55%isexcretedintotheurineinunchangedform[5].PharmacokineticsofSpectinomycindihydrochloridepentahydrateinRat[5]ParameterC0(μg/mL)AUC0-∞(μg?h/mL)Vd(L/kg)CL(L/h/kg)MRT(h)T1/2α(h)T1/2β(h)T1/2γ(h)feCLrenal(L/h/kg)EratioNonatrioventricularanalysis44.316.80.7560.6020.757///0.5530.3591.00Three-compartmentmodel37.815.70.7470.6491.11/0.2370.75419.5//AnimalModel:ArborAcresplusbroilerchicks(15-day-old)[4]Dosage:20mg/kg,60mg/kg,100mg/kgAdministration:Intramuscularinjection(chestmuscles);9daysResult:Showedbiosecurityof20mg/kgbycompletebloodcount,biochemicalparameters,histopathological,clinicalsigns,bodyweightgain,andfeedconversionratio(FCR).Resultedminortoxicityof60mg/kg.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?BMCVetRes.2022Jul12;18(1):270.?Patent.US20200368199A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KhanEA,etal.Safetyevaluationstudyoflincomycinandspectinomycinhydrochlorideintramuscularinjectioninchickens.ToxicolRep.2022Jan29;9:204-209.[2].DaviesJ,etal.Inhibitionofproteinsynthesisbyspectinomycin.Science.1965Sep3;149(3688):1096-8.[3].BrinkMF,etal.SpectinomycininteractsspecificallywiththeresiduesG1064andC1192in16SrRNA,therebypotentiallyfreezingthismoleculeintoaninactiveconformation.NucleicAcidsRes.1994Feb11;22(3):325-31.[4].ParkIK,etal.Spectinomycininhibitstheself-splicingofthegroup1intronRNA.BiochemBiophysResCommun.2000Mar16;269(2):574-9.[5].MadhuraDB,etal.Pharmacokineticprofileofspectinomycininrats.Pharmazie.2013Aug;68(