Oritavancin  (Synonyms: LY 333328; Orbactiv)

Oritavancin (LY 333328), a semisynthetic derivative of Vancomycin (HY-B0671), is an orally active glycopeptide antibiotic with bactericidal activity against gram-positive organisms. Oritavancin shows antibacterial effect against B. anthracis, such as Ames strain with a MIC value of 0.015 g/mL. Oritavancin inhibits cell wall synthesis and disrupts the membrane potential. Oritavancin inhibits ArlS kinase activity thereby interfering the signal transduction. Oritavancin enters cells by adsorptive endocytosis, which drives it to lysosomes, where it exerts antibiotic activity^{[1][2][3][4][5]}.

Oritavancin (25 μM, 30 分钟) 剂量依赖性地抑制体外 98% 的 ArlS (3 μg) 激酶活性，IC⁵⁰ 值为5.47 μΜ^[1]。
Oritavancin (0.7 μM, 42 小时) 降低了 USA300-Pspx 菌株中 spx 的表达^[1]。
Oritavancin (3.1 μM, 24 小时) 破坏成熟的 MRSA 生物膜，促进 Oritavancin 和 Oxacillin (HY-B0925A) 对嵌入的 S. aureus 细胞的杀菌活性^[1]。
Oritavancin (0-80 μg/mL, 2 小时) 细胞外孵育浓度的增加和细胞的摄取在 J774 巨噬细胞中以合作的方式进行^[2]。
Oritavancin (25 mg/L , 24 小时) 对胞内 S. aureus 有明显的杀菌作用^[2]。

Oritavancin 在不同细胞类型中的积累^[2]

(细胞在含 10% FCS 的培养基中，以 25 mg/L 的药物在 37℃ 下孵育 2 小时)^[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Oritavancin (腹腔注射 1 和 3 mg/kg 或静脉注射 15 和 50 mg/kg, 每 48 小时一次连用 14 天或单剂量连用 30 天) 对小鼠吸入性炭疽模型具有显著的保护作用^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1793.10

C₈₆H₉₇Cl₃N₁₀O₂₆

171099-57-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bai J, et al. The role of ArlRS in regulating oxacillin susceptibility in methicillin-resistant Staphylococcus aureus indicates it is a potential target for antimicrobial resistance breakers[J]. Emerg Microbes Infect. 2019;8(1):503-515.  [Content Brief]

  [2]. Van Bambeke F, et al. Cellular pharmacokinetics and pharmacodynamics of the glycopeptide antibiotic oritavancin (LY333328) in a model of J774 mouse macrophages[J]. Antimicrob Agents Chemother. 2004 Aug;48(8):2853-60.  [Content Brief]

  [3]. Heine HS, et al. Efficacy of oritavancin in a murine model of Bacillus anthracis spore inhalation anthrax. Antimicrob Agents Chemother. 2008 Sep;52(9):3350-7.  [Content Brief]

  [4]. Coyle EA, et al. Activity of oritavancin (LY333328), an investigational glycopeptide, compared to that of vancomycin against multidrug-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model. Antimicrob Agents Chemother. 2001 Mar;45(3):706-9.  [Content Brief]

  [5]. Arhin FF, et al. Effect of polysorbate 80 on oritavancin binding to plastic surfaces: implications for susceptibility testing. Antimicrob Agents Chemother. 2008 May;52(5):1597-603.  [Content Brief]