盐酸达巴万星作用机制 - Medchemexpress - MCE中国

1、Product Data SheetDalbavancin hydrochlorideCat. No.: HY-17586CAS No.: 2227366-51-8分式: CHClNO分量: 1853.15作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 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制备储备液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

3、的实验动物和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: 2.08 mg/mL (1.12 mM); Clear solution此案可获得 2.08 mg/mL (1.12 mM，饱和

4、度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 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: 2.08 mg/mL (1.12 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (1.12 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 10

5、0 L 20.8 mg/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: 2.08 mg/mL (1.12 mM); Clear solution; Need warming此案可获得 2.08 mg/mL (1.12 mM) 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 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Dalbavanci

6、n hydrochloride(MDL-63397 hydrochloride)种半合成的脂糖肽抗素，对兰阳性细菌具有有效的杀 活性。Dalbavancin hydrochloride 抑制g/mL12。葡萄球菌和炭疽芽孢杆菌的 MIC90 分别为 0.06 g/mL 和 0.25 体外研究 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.体内研究 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.户使本产品发表的科研献 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