達托霉素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetDaptomycinCat. No.: HY-B0108CAS No.: 103060-53-3分式: CHNO分量: 1620.67作靶點: Bacterial作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (61.70 mM)H2O : 100 mg/mL (61.70 mM; Need ultrasonic)* means soluble, but saturation

2、unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 0.6170 mL 3.0851 mL 6.1703 mL5 mM 0.1234 mL 0.6170 mL 1.2341 mL10 mM 0.0617 mL 0.3085 mL 0.6170 mL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，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和

3、給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 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 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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: 2.5 mg/mL (1.54 mM); Clear solution此案可獲得 2.5 mg/mL (1.54 mM，飽和度未知) 的澄清

4、溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (1.54 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (1.54 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 m

5、g/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (1.54 mM); Clear solution此案可獲得 2.5 mg/mL (1.54 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Daptomycin種脂肽類抗素，具有體外快速殺除蘭陽性細菌

6、的活性。體外研究 Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistantstaphylococci (MIC90 less than or equal to 0.5 mg/L) and against enterococci (MIC90 less than or equal to 2.0 mg/L).Daptomycin is more active than vancomycin against the majorit

7、y of isolated tested. With the exception oftrimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the mostactive against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when theinoculum is increased from 105

8、 to 107 cfu/mL1. Daptomycin is effective within a very narrow range of drugconcentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis2.Daptomycin inhibits the formation of these nucleotide-linked intermediates3.體內(nèi)研究 At a dose of 10 mg/kg given twice dai

9、ly, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its a

10、ctivity iscomparable to that of vancomycin or vancomycin-gentamicin given twice daily2.PROTOCOLAnimal Inocula containing 109 CFU/mL are prepared from an 18-h brain heart infusion broth culture. The exact number inAdministration 2 each inoculum is subsequently determined by the standard serial 10-fol

11、d dilution agar pour plate technique. Animalsare challenged intravenously with a 1.0-mL inoculum. This inoculum is known to infect the renal medulla of normalrats. Twenty-four hours later the animals are divided into eight groups and are given either saline only (controls) orantibiotic therapy initi

12、ated with Daptomycin at 10 mg/kg (Daptomycin10), Daptomycin at 20 mg/kg (Daptomycin20),Daptomycin10 plus gentamicin at 1.5 mg/kg, vancomycin at 20 mg/kg, vancomycin at 20 mg/kg plus gentamicin at1.5 mg/kg, ampicillin at 30 mg per rat per injection, and ampicillin at 30 mg per rat plus gentamicin at

13、1.5 mg/kg.Animals receive Daptomycin20 once daily; all other drugs are administered twice daily. Vancomycin and Daptomycinare given subcutaneously; ampicillin and gentamicin are given intramuscularly. Drugs are administered for up to 13days.MCE has not independently confirmed the accuracy of these m

14、ethods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. Int J Med Microbiol. 2020 Jan.Page 2 of 3 www.MedChemE Diagn Micr Infec Dis. 2020 Mar.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Benson CA, et al. Comparative in-vitr

15、o activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. JAntimicrob Chemother. 1987 Aug;20(2):191-6.2. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203.3. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31