Oritavancin (phosphate)
(Synonyms: 奥利万星二磷酸盐; LY333328 diphosphate) 目录号 : GC44515
A semisynthetic glycopeptide antibiotic
Cas No.:192564-14-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oritavancin is a semisynthetic glycopeptide antibiotic that inhibits the growth of Gram-positive bacteria. It inhibits transglycosylation and transpeptidation in the bacterial cell wall to disrupt membrane integrity. Oritavancin inhibits the growth of clinical isolates from skin and soft-tissue infections, including methicillin-resistant and -susceptible S. aureus (MRSA, MSSA), vancomycin-resistant and -susceptible E. faecium (VREF, VSRF), as well as other staphylococci, streptococci, and enterococci (MIC90s = ≤0.008-0.5 mg/L). Oritavancin inhibits growth of S. aureus in a neutropenic-mouse thigh model of infection (ED50 = 0.95 mg/kg for a single dose). It improves survival in a mouse inhalation model of B. anthracis Ames anthrax when administered prophylactically pre- and postexposure and when administered post symptom development. Formulations containing oritavancin have been used to treat bacterial skin infections.
| Cas No. | 192564-14-0 | SDF | |
| 别名 | 奥利万星二磷酸盐; LY333328 diphosphate | ||
| 分子式 | C86H97Cl3N10O26•2H3PO4 | 分子量 | 1989.1 |
| 溶解度 | 50 mg/mL in DMSO ( Need ultrasonic); 50 mg/mL in Water(Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5027 mL | 2.5137 mL | 5.0274 mL |
| 5 mM | 0.1005 mL | 0.5027 mL | 1.0055 mL |
| 10 mM | 0.0503 mL | 0.2514 mL | 0.5027 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
New Gram-Positive Agents: the Next Generation of Oxazolidinones and Lipoglycopeptides
J Clin Microbiol 2016 Sep;54(9):2225-32.PMID:26962092DOI:10.1128/JCM.03395-15.
The growing problem of antimicrobial resistance among bacterial pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), has reached a critical state. Tedizolid phosphate, dalbavancin, and Oritavancin have recently been approved by the U.S. Food and Drug Administration (FDA) for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and represent the next generation of oxazolidinones and lipoglycopeptides. All three agents exhibit in vitro activity and clinical efficacy against MRSA. Tedizolid phosphate and Oritavancin demonstrate in vitro activity against VRE. These new Gram-positive agents are reviewed here.
Oritavancin binds to isolated protoplast membranes but not intact protoplasts of Staphylococcus aureus
J Mol Biol 2009 Aug 14;391(2):414-25.PMID:19538971DOI:10.1016/j.jmb.2009.06.033.
Solid-state NMR has been used to examine the binding of N'-4-[(4-fluorophenyl)benzyl)]chloroeremomycin, a fluorinated analogue of Oritavancin, to isolated protoplast membranes and whole-cell sucrose-stabilized protoplasts of Staphylococcus aureus, grown in media containing [1(13)C]glycine and L-[epsilon-(15)N]lysine. Rotational-echo double-resonance NMR was used to characterize the binding by estimating internuclear distances from (19)F of Oritavancin to (13)C and (15)N labels of the membrane-associated peptidoglycan and to the (31)P of the phospholipid bilayer of the membrane. In isolated protoplast membranes, both with and without 1 M sucrose added to the buffer, the nascent peptidoglycan was extended away from the membrane surface and the Oritavancin hydrophobic side chain was buried deep in the exposed lipid bilayer. However, there was no N'-4-[(4-fluorophenyl)benzyl)]chloroeremomycin binding to intact sucrose-stabilized protoplasts, even though the drug bound normally to the cell walls of whole cells of S. aureus in the presence of 1 M sucrose. As shown by the proximity of peptidoglycan-bridge (13)C labels to phosphate (31)P, the nascent peptidoglycan of the intact protoplasts was confined to the membrane surface.
Comparative In Vitro Activities of New Antibiotics for the Treatment of Skin Infections
Clin Infect Dis 2019 Apr 8;68(Suppl 3):S200-S205.PMID:30957168DOI:10.1093/cid/ciz003.
Bacterial skin infections result in significant morbidity and have contributed to enhanced health-care resource utilization. The problem is heightened by emerging antimicrobial resistance. Multiple novel agents active against resistant pathogens that cause skin infections-including dalbavancin, tedizolid phosphate, Oritavancin, and delafloxacin-have been approved over the past 5 years. Common features of these agents include gram-positive activity and favorable safety. Of these agents, delafloxacin is unique in being active against both gram-positive and gram-negative pathogens that cause skin infections, including those resistant to other antimicrobial agents. It is, therefore, an effective option for the treatment of skin infections.
Current and future trends in antibiotic therapy of acute bacterial skin and skin-structure infections
Clin Microbiol Infect 2016 Apr;22 Suppl 2:S27-36.PMID:27125562DOI:10.1016/S1198-743X(16)30095-7.
In 2013 the US Food and Drug Administration (FDA) issued recommendations and guidance on developing drugs for treatment of skin infection using a new definition of acute bacterial skin and skin-structure infection (ABSSSI). The new classification includes cellulitis, erysipelas, major skin abscesses and wound infection with a considerable extension of skin involvement, clearly referring to a severe subset of skin infections. The main goal of the FDA was to better identify specific infections where the advantages of a new antibiotic could be precisely estimated through quantifiable parameters, such as improvement of the lesion size and of systemic signs of infection. Before the spread and diffusion of methicillin-resistant Staphylococcus aureus (MRSA) in skin infections, antibiotic therapy was relatively straightforward. Using an empiric approach, a β-lactam was the preferred therapy and cultures from patients were rarely obtained. With the emergence of MRSA in the community setting, initial ABSSSI management has been changed and readdressed. Dalbavancin, Oritavancin and tedizolid are new drugs, approved or in development for ABSSSI treatment, that also proved to be efficient against MRSA. Dalbavancin and Oritavancin have a long half-life and can be dosed less frequently. This in turn makes it possible to treat patients with ABSSSI in an outpatient setting, avoiding hospitalization or potentially allowing earlier discharge, without compromising efficacy. In conclusion, characteristics of long-acting antibiotics could represent an opportunity for the management of ABSSSI and could profoundly modify the management of these infections by reducing or in some cases eliminating both costs and risks of hospitalization.
Early clinical assessment of response to treatment of skin and soft-tissue infections: how can it help clinicians? Perspectives from Europe
Int J Antimicrob Agents 2016 Aug;48(2):127-36.PMID:27283729DOI:10.1016/j.ijantimicag.2016.04.023.
Skin and soft-tissue infections (SSTIs) are a common indication for antibiotic use in Europe and are associated with considerable morbidity. Treatment of SSTIs, occasionally complicated by infection with meticillin-resistant Staphylococcus aureus, can be resource intensive and lead to high healthcare costs. For patients treated in an inpatient setting, once the acute infection has been controlled, a patient may be discharged on suitable oral antibiotic therapy or outpatient parenteral antibiotic therapy. The recently confirmed efficacy of single-dose (e.g. Oritavancin) and two-dose (e.g. dalbavancin) infusion therapies as well as tedizolid phosphate, a short-duration therapy available both for intravenous (i.v.) and oral use, for treating SSTIs has highlighted the need for clinicians to re-evaluate their current treatment paradigms. In addition, recent clinical trial data reporting a novel endpoint of early clinical response, defined as change in lesion size at 48-72 h, may be of value in determining which patients are most suitable for early de-escalation of therapy, including switch from i.v. to oral antibiotics, and subsequent early hospital discharge. The aim of this paper is to review the potential impact of assessing clinical response on clinical decision-making in the management of SSTIs in Europe, with a focus on emerging therapies.