Imipenem (hydrate)
(Synonyms: 亚胺培南一水物; N-Formimidoyl thienamycin monohydrate; MK0787 monohydrate) 目录号 : GC43898
A β-lactam antibiotic
Cas No.:74431-23-5
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
Imipenem monohydrate, a member of the carbapenem class of antibiotics isolated from the soil organism Streptomyces cattleya[1], is an intravenous β-lactam antibiotic effective against a wide range of Gram-positive and Gram-negative bacteria, including several multi-drug resistant bacterial species. Imipenem acts as cell wall-targeting antibiotic[2][3].
References:
[1]. Zhanel GG, et al. Imipenem and meropenem: Comparison of in vitro activity, pharmacokinetics, clinical trials and adverse effects. Can J Infect Dis. 1998 Jul;9(4):215-28.
[2]. Jacoby GA, et al. AmpC beta-lactamases. Clin Microbiol Rev. 2009 Jan;22(1):161-82.
[3]. Balibar CJ, et al. cwrA, a gene that specifically responds to cell wall damage in Staphylococcus aureus. Microbiology. 2010 May;156(Pt 5):1372-83.
| Cas No. | 74431-23-5 | SDF | |
| 别名 | 亚胺培南一水物; N-Formimidoyl thienamycin monohydrate; MK0787 monohydrate | ||
| Canonical SMILES | [H][C@@]1([C@@]([H])([C@H](O)C)C2=O)N2C(C(O)=O)=C(SCCNC=N)C1.O | ||
| 分子式 | C12H17N3O4S•H2O | 分子量 | 317.4 |
| 溶解度 | PBS (pH 7.2): 2 mg/ml | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1506 mL | 15.753 mL | 31.506 mL |
| 5 mM | 0.6301 mL | 3.1506 mL | 6.3012 mL |
| 10 mM | 0.3151 mL | 1.5753 mL | 3.1506 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。
Sitafloxacin hydrate for bacterial infections
Drugs Today (Barc) 2008 Jul;44(7):489-501.PMID:18806900DOI:10.1358/dot.2008.44.7.1219561.
Sitafloxacin hydrate (DU-6859a, Gracevit), a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin has also demonstrated activity against clinical isolates of Klebsiella pneumoniae (including about 67% of strains producing extended-spectrum, beta-lactamases and resistant to ciprofloxacin), Enterobacter cloacae, Pseudomonas aeruginosa with some activity against quinolone-resistant strains and Acinetobacter baumannii. The in vitro activity against anaerobes is comparable to Imipenem or metronidazole. In a published phase II randomized, open-label, multicenter study of patients hospitalized with pneumonia, sitafloxacin (400 mg once daily) was comparable to Imipenem/cilastatin (500 mg three times a day). Results of the phase III trials of sitafloxacin are not available in English. The clinical safety profile of sitafloxacin has been characterized from 1,059 patients who participated in 10 clinical trials. The most common events with 50 or 100 mg twice daily were gastrointestinal disorders (17.2%), mostly diarrhea, and abnormal laboratory test results (16.2%), mostly liver enzyme elevations. For Japanese patients, sitafloxacin provides the broad-spectrum coverage promised by clinafloxacin and trovafloxacin and comparable to carbapenems. While it is currently limited by its potential for phototoxicity in Caucasians, phototoxicity is essentially irrelevant if sitafloxacin is used in hospitals and especially in intensive care units.
Effects of Imipenem-containing Niosome nanoparticles against high prevalence methicillin-resistant Staphylococcus Epidermidis biofilm formed
Sci Rep 2022 Mar 24;12(1):5140.PMID:35332241DOI:10.1038/s41598-022-09195-9.
We aim to assess the antibacterial and anti-biofilm properties of Niosome-encapsulated Imipenem. After isolating Staphylococcus epidermidis isolates and determining their microbial sensitivity, their ability to form biofilms was examined using plate microtiter assay. Various formulations of Niosome-encapsulated Imipenem were prepared using the thin-film hydration method, Minimum Biofilm Inhibitory Concentration (MBIC) and Minimum Inhibitory Concentration (MIC) were determined, and biofilm genes expression was examined. Drug formulations' toxicity effect on HDF cells were determined using MTT assay. Out of the 162 separated S. epidermidis, 106 were resistant to methicillin. 87 MRSE isolates were vancomycin-resistant, all of which could form biofilms. The F1 formulation of niosomal Imipenem with a size of 192.3 ± 5.84 and an encapsulation index of 79.36 ± 1.14 was detected, which prevented biofilm growth with a BGI index of 69% and reduced icaD, FnbA, EbpS biofilms' expression with P ≤ 0.001 in addition to reducing MBIC and MIC by 4-6 times. Interestingly, F1 formulation of niosomal Imipenem indicated cell viability over 90% at all tested concentrations. The results of the present study indicate that Niosome-encapsulated Imipenem reduces the resistance of MRSE to antibiotics in addition to increasing its anti-biofilm and antibiotic activity, and could prove useful as a new strategy for drug delivery.
Acute pancreatitis
Am Fam Physician 2014 Nov 1;90(9):632-9.PMID:25368923doi
Acute pancreatitis is most commonly caused by gallstones or chronic alcohol use, and accounts for more than 200,000 hospital admissions annually. Using the Atlanta criteria, acute pancreatitis is diagnosed when a patient presents with two of three findings, including abdominal pain suggestive of pancreatitis, serum amylase and/or lipase levels at least three times the normal level, and characteristic findings on imaging. It is important to distinguish mild from severe disease because severe pancreatitis has a mortality rate of up to 30%. Contrast-enhanced computed tomography is considered the diagnostic standard for radiologic evaluation of acute pancreatitis because of its success in predicting disease severity and prognosis. The BALI and computed tomography severity index scores also can aid in determining disease severity and predicting the likelihood of complications. Treatment begins with pain control, hydration, and bowel rest. In the first 48 to 72 hours of treatment, monitoring is required to prevent morbidity and mortality associated with worsening pancreatitis. When prolonged bowel rest is indicated, enteral nutrition is associated with lower rates of complications, including death, multiorgan failure, local complications, and systemic infections, than parenteral nutrition. In severe cases involving greater than 30% necrosis, antibiotic prophylaxis with Imipenem/cilastatin decreases the risk of pancreatic infection. In gallstone-associated pancreatitis, early cholecystectomy and endoscopic retrograde cholangiopancreatography with sphincterotomy can decrease length of hospital stay and complication rates. A multidisciplinary approach to care is essential in cases involving pancreatic necrosis.
Recognition of Imipenem and meropenem by the RND-transporter MexB studied by computer simulations
J Am Chem Soc 2012 Nov 21;134(46):19146-58.PMID:23146101DOI:10.1021/ja307803m.
Basic understanding of the means by which multidrug efflux systems can efficiently recognize and transport drugs constitutes a fundamental step toward development of compounds able to tackle the continuous outbreak of new bacterial strains resistant to traditional antibiotics. We applied a series of computational techniques, from molecular docking to molecular dynamics simulations and free energy estimate methods, to determine the differences in the binding properties of Imipenem and meropenem, two potent antibiotics of the carbapenem family, to MexB, the RND transporter of the major efflux system of Pseudomonas aeruginosa. We identified and characterized two affinity sites in the periplasmic domain of the transporter, sharing strong similarities with the distal and proximal binding pockets identified in AcrB, the homologue of MexB in Escherichia coli. According to our results, meropenem has a higher affinity to the distal binding pocket than Imipenem while both compounds are weakly bound to the proximal pocket. This different behavior is mainly due to the hydration properties of the nonpharmacophore part of the two compounds, being that of Imipenem less bulky and hydrophobic. Our data provide for the first time a rationale at molecular level for the experimental evidence indicating meropenem as a compound strongly affected by MexB contrary to Imipenem, which is apparently poorly transported by the same pump.
Interaction between capecitabine and brivudin in a patient with breast cancer
Nat Rev Clin Oncol 2010 Jan;7(1):55-8.PMID:20029444DOI:10.1038/nrclinonc.2009.185.
Background: A 66-year-old woman with metastatic mammary carcinoma, who was being treated with capecitabine, contracted a herpes zoster infection that was treated with the antiviral drug brivudin. A drug-drug interaction between brivudin and capecitabine caused medullar aplasia, serious toxic effects to the intestinal mucous membrane, hand-foot syndrome, onycholysis and dental pigmentation. Investigations: Physical examination, blood analysis, blood cultures, chest X-ray, bone marrow aspiration and biopsy. Diagnosis: Serious adverse event secondary to inhibition of dihydropyrimidine dehydrogenase by a drug-drug interaction between capecitabine and brivudin. Management: Intravenous hydration, Imipenem, red blood cell and platelet transfusions, filgrastim, omeprazole, care of the mouth and feet, topical anesthetics, systemic analgesics and parenteral nutrition.