达托霉素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetDaptomycinCat. No.: HY-B0108CAS No.: 103060-53-3分式: CHNO分量: 1620.67作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 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制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和

3、给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (1.54 mM); Clear solution此案可获得 2.5 mg/mL (1.54 mM，饱和度未知) 的澄清

4、溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (1.54 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (1.54 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 m

5、g/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (1.54 mM); Clear solution此案可获得 2.5 mg/mL (1.54 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Daptomycin种脂肽类抗素，具有体外快速杀除兰阳性细菌

6、的活性。体外研究 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.体内研究 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.户使本产品发表的科研献 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