Oritavancin
Based on 3 publication(s) in Google Scholar
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.
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- CAS 番号: 171099-57-3
- 分子式: C86H97Cl3N10O26
- 分子量:1793.10
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Oritavancin
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生物活性
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Glycopeptide |
Oritavancin (25 μM, 30 min) dose-dependently inhibits the kinase activity of ArlS (3 μg) by 98% with an IC50 value of 5.47 μΜ in vitro[1].
Oritavancin (0.7 μM, 42 h) decreases spx expression in the USA300-Pspx strain[1].
Oritavancin (3.1 μM, 24 h) disrupts mature MRSA biofilms and facilitates bactericidal activity of Oritavancin and Oxacillin (HY-B0925A) against embedded S. aureus cells[1].
Oritavancin’ (0-80 μg/mL, 2 h) incubation with increasing extracellular concentrations and the uptake by cells proceed in an cooperative manner in J774 macrophages[2].
Oritavancin (25 mg/L, 24 h) exerts a marked bactericidal effect against intracellular S. aureus[2].
Oritavancin accumulation by different cell types[2]
(The cells were incubated for 2 h at 37°C with 25 mg of the drug per liter in a medium containing 10% FCS)[2]
| Cell type | Accumulation ratio (no. of determinations) |
| J774 mouse macrophages | 66.4±11.8 (12) |
| THP-1 human monocytes | 84.3±7.0 (9) |
| Rat embryo fibroblasts | 72.4±9.4 (6) |
| LLC-PK1 pig kidney proximal tubular cells | 37.8±6.4 (3) |
| Caco-2 human colorectal cells. | 13.8±0.4 (3) |