鹽酸達巴萬星作用機制 - Medchemexpress - MCE中國

1、Product Data SheetDalbavancin hydrochlorideCat. No.: HY-17586CAS No.: 2227366-51-8分式: CHClNO分量: 1853.15作靶點: Bacterial作通路: Anti-infection儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 50 mg/mL (26.98 mM; Need ultrasonic)DMSO : 24 mg/mL (12.95 mM)* means soluble, but satur

2、ation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 0.5396 mL 2.6981 mL 5.3962 mL5 mM 0.1079 mL 0.5396 mL 1.0792 mL10 mM 0.0540 mL 0.2698 mL 0.5396 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

3、的實驗動物和給藥式選擇適當?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: 2.08 mg/mL (1.12 mM); Clear solution此案可獲得 2.08 mg/mL (1.12 mM，飽和

4、度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 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: 2.08 mg/mL (1.12 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (1.12 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 10

5、0 L 20.8 mg/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: 2.08 mg/mL (1.12 mM); Clear solution; Need warming此案可獲得 2.08 mg/mL (1.12 mM) 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 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Dalbavanci

6、n hydrochloride(MDL-63397 hydrochloride)種半合成的脂糖肽抗素，對蘭陽性細菌具有有效的殺 活性。Dalbavancin hydrochloride 抑制g/mL12。葡萄球菌和炭疽芽孢桿菌的 MIC90 分別為 0.06 g/mL 和 0.25 體外研究 Dalbavancin is a parenterally administered semisynthetic lipoglycopeptide developed to combat infections caused byresistant gram-positive pathogens. Dalb

7、avancin exhibits potent in vitro bactericidal activity against gram-positivepathogens including S. aureus (MRSA), VISA, and non-VanA strains of VRE. Dalbavancin is developed for thetreatment of complicated skin and skin structure infections (cSSSIs), predominantly those caused by MRSA and -hemolytic

8、 streptococci, organisms against which it has shown greater potency than existing glycopeptide therapeuticagents12.體內(nèi)研究 Dalbavancin (15-240 mg/kg; intraperitoneal injection; every 36 h or 72 h; for 14 days; female BALB/c mice) treatmenthas a survival rate of 80% to 100% of mice with all dose regimen

9、s1.Animal Model: Female BALB/c mice (6-8 weeks) challenged with Ames strain of B. anthracis1Dosage: 15 mg/kg, 30 mg/kg, 60 mg/kg, 120 mg/kg, 240 mg/kgAdministration: Intraperitoneal injection; every 36 h or 72 h; for 14 daysResult: The efficacy was 80 to 100%, as determined by the rate of survival a

10、t 42 days, whentreatment was initiated 24 h postchallenge with regimens of 15 to 120 mg/kg every36 h or 30 to 240 mg/kg every 72 h.戶使本產(chǎn)品發(fā)表的科研獻 Antivir Res. 2020 Apr. J Antibiot (Tokyo). 2019 Feb;72(2):114-117.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Heine HS,

11、et al. Activity of dalbavancin against Bacillus anthracis in vitro and in a mouse inhalation anthrax model. Antimicrob Agents Chemother. 2010Mar;54(3):991-6.Page 2 of 3 www.MedChemE2. Bennett JW, et al. Dalbavancin in the treatment of complicated skin and soft-tissue infections: a review. Ther Clin Risk Manag. 2008 Feb;4(1):31-40.McePdfHeightCaution: Product has not been fully validat