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Davercin Sale

(Synonyms: 环酯红霉素; Erythromycin Cyclocarbonate) 目录号 : GC43381

A macrolide antibiotic

Davercin Chemical Structure

Cas No.:55224-05-0

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1mg
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5mg
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10mg
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25mg
¥3,569.00
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产品描述

Davercin (Erythromycin Cyclocarbonate), derivative of Erythromycin, which is active against Gram-positive and some Gram-negative microorganisms.

Erythromycin is used in treatment of respiratory, gastrointestinal, and genital tract infections, as well as skin and soft tissue infections. Erythromycin, with its ten chiral centers and two sugar substituents (L-cladinose and D-desosamine), is a good starting point for numerous medicinal chemistry efforts for improvement of its biological profile (better activity, higher stability, and improved bioavailability) since the first generation of macrolides, which had low toxicity and good tolerability, are unstable in acidic media, had low toxicity and good tolerability[1].

References:
[1]. Jelic D, et al. From Erythromycin to Azithromycin and New Potential Ribosome-Binding Antimicrobials. Antibiotics (Basel). 2016 Sep 1;5(3). pii: E29.

Chemical Properties

Cas No. 55224-05-0 SDF
别名 环酯红霉素; Erythromycin Cyclocarbonate
Canonical SMILES C[C@H]1[C@H](O)[C@@](OC)(C)C[C@@](O[C@H]([C@@H](C)C(O[C@H](CC)[C@]2(C)[C@@](OC(O2)=O)([H])[C@H]3C)=O)[C@H](C)[C@@H](O[C@@]4([H])[C@H](O)[C@@H](N(C)C)C[C@@H](C)O4)[C@](C)(O)C[C@@H](C)C3=O)([H])O1
分子式 C38H65NO14 分子量 759.9
溶解度 DMF: 15 mg/ml,DMSO: 15 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml 储存条件 Store at -20°C
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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。
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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.316 mL 6.5798 mL 13.1596 mL
5 mM 0.2632 mL 1.316 mL 2.6319 mL
10 mM 0.1316 mL 0.658 mL 1.316 mL
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Research Update

[Comparative studies of cyclic 11, 12 erythromycin carbonate (Davercin) and erythromycin a levels in lung tissue, serum and bronchial secretions]

Pneumonol Pol 1989 Jan;57(1):25-8.PMID:2813147doi

A comparison of serum, pulmonary tissue and bronchial secretory levels of erythromycin and cyclic--11,12 carbonate of erythromycin (Davercin--Polfa) was carried out in 55 patients with lung cancer. All patients received erythromycin and Davercin 80 hours prior surgery, during which a small fragment of pulmonary tissue was removed for further evaluation. Concentration of both antibiotics was determined microbiologically. Better penetration of Davercin to the pulmonary tissue was found, as well as higher tissue concentration. The study demonstrates the advantage of Davercin over erythromycin in treating bacterial infections of the respiratory system.

Comparative efficacy of new investigational agents against Helicobacter pylori

Aliment Pharmacol Ther 2001 Apr;15(4):487-92.PMID:11284777DOI:10.1046/j.1365-2036.2001.00957.x.

Background: Emergence of antibiotic resistant Helicobacter pylori has necessitated the identification of alternate therapies for the treatment of this infection. Aim: To assess the in vitro efficacy of two investigational agents: DMG-MINO CL 344 (a N,N-dimethylglycylamido derivative of minocycline), and Davercin, a cyclic carbonate of erythromycin A as compared to older antibiotics (clarithromcyin, azithromycin, minocycline, tetracycline, ofloxacin, ciprofloxacin, cefixime) against clinical isolates of H. pylori. Methods: Testing was performed using the agar dilution method approved by the NCCLS subcommittee on antimicrobial susceptibility testing, Helicobacter pylori working group. Under these guidelines, Mueller-Hinton agar containing 5% aged sheep blood was used. All incubations were done under CampyPak Plus conditions for 72 h at 37 degrees C. The drug concentrations in the agar ranged from 0.016 to 16 microg/mL. Twenty-one clarithromycin-resistant and 16 clarithromycin-susceptible clinical isolates of H. pylori obtained from patients with duodenal ulcer were used. H. pylori ATCC 43504 was used as the control in all determinations. Results: Against clarithromycin susceptible isolates, all antimicrobial agents except the fluoroquinolones were highly effective. Against clarithromycin-resistant H. pylori, the MIC50/MIC90 values showed that the tetracyclines and cefixime were the most efficacious agents. The fluoroquinolones and macrolides were ineffective. Macrolide cross-resistance was detected. Conclusion: Macrolide cross-resistance prevents the use of this entire class of antimicrobials when clarithromycin resistance is present. Tetracyclines and cefixime are possible alternative agents for the treatment of H. pylori infection in these patients.

[Anaerobic microbes in perimandibular inflammation]

Rev Stomatol Chir Maxillofac 1984;85(6):484-7.PMID:6596693doi

Studies conducted in 16 patients with perimandibular inflammation included bacteriological examinations and tests of the resistance of the bacterial flora to 6 antibiotics:Davercin, erythromycine, penicillin, ampicillin, tetracycline and chloramphenicol. A total of 73 strains (47 anaerobic and 26 aerobic) were isolated, including 47 Gram - and 26 Gram's strain +. Anaerobic Gram - ve bacteria appear to be the principal cause of perimandibular inflammatory lesions, streptococcus viridans being identified more frequently in these cases than in the normal buccal cavity. Bacterial flora of dental origin was more sensitive to Davercin than to the other 5 antibiotics tested.

[Analysis of the infection status and the drug resistance of mycoplasma and chlamydiae in genitourinary tracts of children with suspected nongonococcal urethritis]

Zhonghua Er Ke Za Zhi 2009 Jan;47(1):62-4.PMID:19573386doi

Objective: To investigate the infection and the drug resistance status of mycoplasma and chlamydiae in genitourinary tracts of children with suspected nongonococcal urethritis (NGU) and provide information for clinical rational administration of antimicrobial agents. Methods: Samples of genitourinary tract secretion from 146 children who were suspected of having nongonococcal urethritis or colpitis were collected and tested for mycoplasma via culture and for chlamydia with antigen detection. Meanwhile, susceptibility test was carried out on the samples which were positive in mycoplasma cultivation. Chlamydia antigen was detected by the polymer conjugate-enhanced (PCE) indirect enzyme immunoassay (EIA) (IDEIA PCE Chlamydia; DAKO). The mycoplasma culture medium was produced by Nanjing Liming Biological Products Co,. Ltd. Antibiotics used for susceptibility test were erythromycin, roxithromycin, josamycin, leucomycin, meleumycin, rovamycin, azithromycin, clarithromycin, cycloate erythromycin, and clindamycin. Results: Fifteen samples were positive for Chlamydia trachomatis (Ct) by antigen detection (10.3%), 82 samples were positive in mycoplasma cultivation (56.2%), and among the 82 samples, 58 were positive for Ureaplasma urealyticum (Uu, 39.7%), 9 were positive for Mycoplasma hominis (Mh, 6.2%), and 15 were positive for Uu and Mh (10.3%). Of all the samples, 4 were positive for both Uu and Ct (2.7%). The rates of drug resistance of the 10 commonly used antibiotics were as follows: erythromycin 32.9%, roxithromycin 41.5%, josamycin 19.5%, leucomycin 22.0%, meleumycin 28.0%, rovamycin 30.5%, azithromycin 37.8%, clarithromycin 26.8%, Davercin 24.4%, and clindamycin 26.8%, respectively. The results indicated that drug resistance rates of josamycin and leucomycin were the lowest, and the rates of roxithromycin and azithromycin were the highest. Conclusions: The infection rates of mycoplasma and chlamydia in children suspected NGU were high. Mycoplasma showed drug resistance to a different degree to 10 common antibiotics. The results of chemosensitivity showed that josamycin had the highest susceptibility rate.

[Drug sensitivity of bacillus strains M. avium-intracellulare (MAIC), M. kansasii cultured from patients with mycobacteriosis before treatment]

Pneumonol Alergol Pol 1993;61(5-6):248-53.PMID:8348088doi

The aim of study was to evaluate a drug sensitivity of M. avium-intracellulare, M. xenopi and M. kansasii cultured from 55 patients with mycobacterioses. The identification of strains was performed with morphological and biochemical tests and thin-layer chromatography. Resistance tests were done on egg L-J and agar media for selected drugs. It was documented that MAIC strains were non-sensitive on isoniazid and rifampicin, and other ones. The most active drug was cycloserine inhibiting growth of 80% but rifabutine--50% of strains. M. xenopi strains were sensitive for tested drugs including isoniazid and rifampicin (about 30%). M. kansasii strains were in 100% sensitive for cyclosporine, rifabutine, Davercin and ofloxacin and partly for isoniazid, streptomycin and Augmentin.