Dalfopristin (RP54476)
(Synonyms: 达福普汀; RP54476) 目录号 : GC32105
Dalfopristin (RP54476) is a semi-synthetic analogue of ostreogyrcin A. Quinupristin/dalfopristin (Q/D) is a parental streptogramin with a spectrum of activity that includes Gram-positive pathogens, including those resistant to other classes of antimicrobial compounds.
Cas No.:112362-50-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dalfopristin (RP54476) is a semi-synthetic analogue of ostreogyrcin A. Quinupristin/dalfopristin (Q/D) is a parental streptogramin with a spectrum of activity that includes Gram-positive pathogens, including those resistant to other classes of antimicrobial compounds.
[1] Joseph M Blondeau, Stephen E Sanche. Expert Opin Pharmacother. 2002 Sep;3(9):1341-64.
| Cas No. | 112362-50-2 | SDF | |
| 别名 | 达福普汀; RP54476 | ||
| Canonical SMILES | O=S(CCN(CC)CC)([C@H]1[C@@](C(O[C@H]([C@@H](/C=C/C(NC/C=C\C(C)=C\2)=O)C)C(C)C)=O)([H])N(C(C3=COC(CC(C[C@@H]2O)=O)=N3)=O)CC1)=O | ||
| 分子式 | C34H50N4O9S | 分子量 | 690.85 |
| 溶解度 | DMSO : ≥ 3 mg/mL (4.34 mM) | 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 | 1.4475 mL | 7.2375 mL | 14.4749 mL |
| 5 mM | 0.2895 mL | 1.4475 mL | 2.895 mL |
| 10 mM | 0.1447 mL | 0.7237 mL | 1.4475 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。
The global prevalence of Daptomycin, Tigecycline, Quinupristin/Dalfopristin, and Linezolid-resistant Staphylococcus aureus and coagulase-negative staphylococci strains: a systematic review and meta-analysis
Antimicrob Resist Infect Control 2020 Apr 22;9(1):56.PMID:32321574DOI:10.1186/s13756-020-00714-9.
Objective: Methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant coagulase-negative Staphylococcus (MRCoNS) are among the main causes of nosocomial infections, which have caused major problems in recent years due to continuously increasing spread of various antibiotic resistance features. Apparently, vancomycin is still an effective antibiotic for treatment of infections caused by these bacteria but in recent years, additional resistance phenotypes have led to the accelerated introduction of newer agents such as linezolid, tigecycline, daptomycin, and quinupristin/Dalfopristin (Q/D). Due to limited data availability on the global rate of resistance to these antibiotics, in the present study, the resistance rates of S. aureus, Methicillin-resistant S. aureus (MRSA), and CoNS to these antibiotics were collected. Method: Several databases including web of science, EMBASE, and Medline (via PubMed), were searched (September 2018) to identify those studies that address MRSA, and CONS resistance to linezolid, tigecycline, daptomycin, and Q/D around the world. Result: Most studies that reported resistant staphylococci were from the United States, Canada, and the European continent, while African and Asian countries reported the least resistance to these antibiotics. Our results showed that linezolid had the best inhibitory effect on S. aureus. Although resistances to this antibiotic have been reported from different countries, however, due to the high volume of the samples and the low number of resistance, in terms of statistical analyzes, the resistance to this antibiotic is zero. Moreover, linezolid, daptomycin and tigecycline effectively (99.9%) inhibit MRSA. Studies have shown that CoNS with 0.3% show the lowest resistance to linezolid and daptomycin, while analyzes introduced tigecycline with 1.6% resistance as the least effective antibiotic for these bacteria. Finally, MRSA and CoNS had a greater resistance to Q/D with 0.7 and 0.6%, respectively and due to its significant side effects and drug-drug interactions; it appears that its use is subject to limitations. Conclusion: The present study shows that resistance to new agents is low in staphylococci and these antibiotics can still be used for treatment of staphylococcal infections in the world.
Quinupristin/Dalfopristin
Expert Opin Pharmacother 2002 Sep;3(9):1341-64.PMID:12186626DOI:10.1517/14656566.3.9.1341.
Gram-positive pathogens are associated with both community- and hospital-acquired infections. These infections may be life-threatening in hospitalised patients, especially in those with significant underlying acute or chronic diseases. Prompt and appropriate antimicrobial therapy is essential for avoiding morbidity and mortality. The concept of appropriate therapy is being redefined by increasing antimicrobial resistance, especially amongst Gram-positive pathogens. This has been most dramatic with penicillin-resistant Streptococcus pneumoniae in the community, including cross-resistance to other classes of antimicrobial agents. In the US, the incidence of methicillin-resistant Staphylococcus aureus (MRSA) with community isolates is significant. For hospital-acquired Gram-positive pathogens, MRSA, vancomycin-resistant Enterococcus species and vancomycin-intermediate resistant and -resistant S. aureus are a great concern, particularly as the frequency of recovery of these pathogens from infected patients increases. The net result of these various resistance issues is a reduction in the number of appropriate antimicrobial agents for treating infected patients. Quinupristin/Dalfopristin is a parental streptogramin with a spectrum of activity that includes Gram-positive pathogens, including those resistant to other classes of antimicrobial compounds. In this review, data summarising the frequency of recovered Gram-positive pathogens from various infectious diseases, the escalating prevalence of resistance amongst Gram-positive pathogens and the factors making quinupristin/Dalfopristin a suitable agent for treating patients infected with Gram-positive organisms will be discussed.
Quinupristin-dalfopristin: an overview
Pharmacotherapy 2000 Dec;20(12):1469-85.PMID:11130220DOI:10.1592/phco.20.19.1469.34858.
Synercid (RP 59500), the first injectable streptogramin antibiotic, is composed of two semisynthetic pristinamycin derivatives, quinupristin and Dalfopristin. Individually, each component has bacteriostatic activity against staphylococci and streptococci, but together, the agents exhibit synergy, leading to bactericidal activity. The combination drug, however, is bacteriostatic against Enterococcus faecium and has poor activity against Enterococcus faecalis. Despite a short half-life, an extended postantibiotic effect allows the agent to be dosed every 8-12 hours. Both drugs are largely hepatically metabolized and excreted in bile. Although not metabolized by cytochrome P450 3A4, quinupristin-dalfopristin can inhibit agents that are metabolized through this pathway. Dosage adjustments may be necessary in patients with hepatic dysfunction. Alterations in renal function have minimal effects on the agent's pharmacokinetics. Adverse events include arthralgia, myalgias, and infusion-related pain. Based on available data, quinupristin-dalfopristin appears to have a role in treating severely ill patients with infections due to multiresistant gram-positive pathogens.
Quinupristin/Dalfopristin: a therapeutic review
Clin Ther 2001 Jan;23(1):24-44.PMID:11219478DOI:10.1016/s0149-2918(01)80028-x.
Background: The proliferation of multidrug-resistant gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium (VREF), has created a pressing need for effective alternative antibiotics. Quinupristin/Dalfopristin is a new combination streptogramin product with a selective spectrum of antibacterial activity, mainly against gram-positive aerobic bacteria. It has been assessed primarily in emergency-use protocols, in hospitalized patients with skin and skin-structure infections, and in patients with VREF bacteremia. Objectives: The objectives of this review were to summarize important results of in vitro microbiologic studies; to provide information on relevant pharmacokinetic parameters, drug interactions, and Y-site compatibility; and to assess efficacy and safety data from clinical studies of quinupristin/Dalfopristin. Methods: Articles included in this review were identified by a MEDLINE search of the literature published between 1966 and September 2000 using the terms Synercid, quinupristin, and Dalfopristin. Additional articles were retrieved from the reference lists of articles identified in the MEDLINE search. Results: In vitro analysis of the spectrum of activity of quinupristin/Dalfopristin has confirmed its relatively selective coverage of gram-positive aerobic bacteria. Both quinupristin and Dalfopristin undergo hepatic metabolism and are extensively excreted in the feces. Combination quinupristin/Dalfopristin inhibits the cytochrome P450 3A4 pathway, and caution is warranted with concomitant use of other medications eliminated via this pathway. In trials in patients with VREF infections, treatment success with quinupristin/Dalfopristin varied depending on the site of infection, ranging from 51.9% in bacteremia of unknown origin to 88.9% in urinary tract infections. The results of comparative clinical trials suggest that quinupristin/Dalfopristin has similar efficacy to that of commonly used antibiotics, including cefazolin, oxacillin, and vancomycin, in patients with skin and skin-structure infections or nosocomial pneumonia. The most frequently reported adverse effects with administration of quinupristin/Dalfopristin were infusion-site inflammation, pain, and edema; other infusion-site reactions; and thrombophlebitis. Arthralgia, myalgia, nausea, diarrhea, vomiting, and rash occurred in 2.5% to 4.6% of patients and were the most frequently reported systemic adverse events. Conclusions: Outcomes data from clinical trials indicate that quinupristin/Dalfopristin has the potential to play an important role in the treatment of bacteremia, complicated skin and skin-structure infections, and nosocomial pneumonia caused by VREF. Issues of bacterial resistance to quinupristin/Dalfopristin and other appropriate uses of this combination agent remain to be elucidated.
Quinupristin/Dalfopristin: a review of its use in the management of serious gram-positive infections
Drugs 1999 Dec;58(6):1061-97.PMID:10651391DOI:10.2165/00003495-199958060-00008.
Quinupristin/Dalfopristin is the first parenteral streptogramin antibacterial agent, and is a 30:70 (w/w) ratio of 2 semisynthetic pristinamycin derivatives. The combination has inhibitory activity against a broad range of gram-positive bacteria including methicillin-resistant staphylococci, vancomycin-resistant Enterococcus faecium (VREF), drug-resistant Streptococcus pneumoniae, other streptococci, Clostridium perfringens and Peptostreptococcus spp. The combination also has good activity against selected gram-negative respiratory tract pathogens including Moraxella catarrhalis, Legioniella pneumophila and Mycoplasma pneumoniae. Quinupristin/Dalfopristin has poor activity against E. faecalis. The combination is bactericidal against staphylococci and streptococci, although constitutive erythromycin resistance can affect its activity. As for many other agents, quinupristin/Dalfopristin is generally bacteriostatic against E. faecium. In patients with methicillin-resistant S. aureus (MRSA) or VREF infections participating in prospective emergency-use trials, quinupristin/Dalfopristin 7.5 mg/kg every 8 or 12 hours achieved clinical or bacteriological success in > or =64% of patients. Emergence of resistance to quinupristin/Dalfopristin was uncommon (4% of patients) in those with VREF infections. Quinupristin/Dalfopristin 7.5 mg/kg 8- or 12-hourly also achieved similar clinical success rates to comparator agents in patients with presumed gram-positive complicated skin and skin structure infections or nosocomial pneumonia (administered in combination with aztreoman) in 3 large multicentre randomised trials. Systemic adverse events associated with quinupristin/Dalfopristin include gastrointestinal events (nausea, vomiting and diarrhoea), rash and pruritus. Myalgias and arthralgias also occur at an overall incidence of 1.3%, although higher rates (2.5 to 31%) have been reported in patients with multiple comorbidities. Venous events are common if the drug is administered via a peripheral line; however, several management options (e.g. use of central venous access, increased infusion volume) may help to minimise their occurrence. Hyperbilirubinaemia has been documented in 3.1% of quinupristin/Dalfopristin recipients versus 1.3% of recipients of comparator agents. Quinupristin/Dalfopristin inhibits cytochrome P450 3A4 and therefore has the potential to increase the plasma concentrations of substrates of this enzyme. Conclusions: Quinupristin/Dalfopristin, the first parenteral streptogramin, offers a unique spectrum of activity against multidrug-resistant gram-positive bacteria. In serious gram-positive infections for which there are other treatment options available, the spectrum of activity and efficacy of quinupristin/ Dalfopristin should be weighed against its tolerability and drug interaction profile. However, in VREF or unresponsive MRSA infections, where few proven treatment options exist, quinupristin/Dalfopristin should be considered as a treatment of choice for these seriously ill patients.