PK150-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPK150Cat.No.:HY-133119CASNo.:2165324-62-7分?式:C??H?ClF?N?O?分?量:394.68作?靶點(diǎn):Bacterial作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(633.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5337mL12.6685mL25.3370mL5mM0.5067mL2.5337mL5.0674mL10mM0.2534mL1.2668mL2.5337mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.27mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.27mM);ClearsolutionBIOLOGICALACTIVITY?物活性PK150?種Sorafenib的類似物。PK150具有?服活性，具有抗活性。PK150抑制甲氧西林敏感??葡萄球(MSSA)，耐甲氧西林??葡萄球(MRSA)，萬古霉素中介??葡萄球(VISA)的MIC分別為0.3，0.3-1，0.3μM[1]。IC50&TargetMIC:0.3μM(MSSA),0.3-1μM(MRSA),0.3μM(VISA)[1]體內(nèi)研究TheinvivoefficacyofPK150againstmethicillin-sensitiveS.aureus(MSSA)(strainSH1000)isdemonstratedinamurinebloodstreaminfectionmodel.PK150(20?mg/kg;p.o.)significantlyreducesbacterialloadsintheliverandheart[1].PK150(10and20mg/kgorally;or10mg/kgintravenously)showsnoobvioussignsoftoxicityinmice.Higheri.v.dosingof20mg/kgresultsinseveretoxiceffectsandisthusavoidedforsubsequenttherapeuticmodels[1].AnimalModel:Pathogen-free9-weekoldfemaleC57BL/6Jmice[1]Dosage:20?mg/kgAdministration:Administeredp.o.Result:Bacterialloadsintheliverandheartwerebothsignificantlyreducedbyapproximately100-fold.AnimalModel:OutbredmaleCD-1mice,4weeksold[1]Dosage:10and20mg/kg(PharmacokineticAnalysis)Administration:Administeredbyintragastricgavageat10and20mg/kgorintravenouslyat10mg/kgResult:Oralbioavailabilitywasapproximately63%andthemeanresidencetimewasslightlyenhancedviathisadministrationroute.T1/2=11.69±1.5,9.67±0.2,and9.37±0.5hoursfor10mg/kgi.v.,10mg/kgp.o.,and20mg/kgp.o.,respectively.REFERENCES[1].LeP,etal.Repurposinghumankinaseinhibitorstocreateanantibioticactiveagainstdrug-resistantStaphylococcusaureus,persistersandbiofilms.NatChem.2019Dec16.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicat