Josamycin (EN-141)
(Synonyms: 交沙霉素; EN-141) 目录号 : GC32108
A macrolide antibiotic
Cas No.:16846-24-5
Sample solution is provided at 25 µL, 10mM.
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Josamycin is a macrolide antibiotic originally isolated from S. narbonensis.1 It is active against clinical isolates of the Gram-positive aerobic bacteria S. aureus, S. epidermidis, S. pneumoniae, S. pyogenes, and S. agalactiae (MIC50s = ≤0.39 ?g/ml for all), as well as the Gram-negative anaerobic bacteria Peptococcus, Peptostreptococcus, and Clostridium when used at concentrations of 6.25 ?g/ml.2 It increases survival in mouse models of systemic S. aureus, S. pyogenes, and S. pneumoniae infection with ED50 values of 206.8, 205, and 86.7 mg/kg, respectively.3
1.Osono, T., Oka, Y., Watanabe, S., et al.A new antibiotic, josamyicn. I. Isolation and physico-chemical characteristicsJ. Antibiot. (Tokyo)20(3)174-180(1967) 2.Reese, R.E., Betts, R.F., Goedde, L.W., et al.In vitro susceptibility of common clinical anaerobic and aerobic isolates against josamycinAntimicrob. Agents Chemother.10(2)253-257(1976) 3.Ono, T., Numata, K., Nagate, T., et al.In vitro and in vivo antibacterial activities of clarithromycinChemotherapy42(3)159-169(1996)
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Kinase experiment: |
Josamycin is prepared in polymix buffer, containing 5 mM magnesium acetate, 5 mM ammonium chloride, 95 mM potassium chloride, 0.5 mM calcium chloride, 8 mM putrescine, 1 mM spermidine, 5 mM potassium phosphate, and 1 mM dithioerythritol. Josamycin at different concentrations (2, 3, 4, and 6 μM is added to preinitiated ribosomes to start the incubation. One volume of elongation mix is added to 1 volume of reaction mix at each incubation time, and after 10 s the reaction is quenched with formic acid. The association rates are estimated from the fraction of tri-peptide-forming ribosomes[1]. |
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Animal experiment: |
Rat: Tritium-labelled Josamycin (200 mg/kg) is orally administrated to rats. The blood and tissue levels are determined at 1 h and 3 h by bioassay[2].Mouse: Tritium-labelled Josamycin (200 mg/kg) is orally administrated to mice. The blood and tissue levels are determined at 1 h and 3 h by bioassay[2]. |
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References: [1]. Lovmar M, et al. Kinetics of macrolide action: the Josamycin and erythromycin cases. J Biol Chem. 2004 Dec 17;279(51):53506-15. |
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| Cas No. | 16846-24-5 | SDF | |
| 别名 | 交沙霉素; EN-141 | ||
| Canonical SMILES | O[C@H]1[C@](O[C@H](C)[C@@H](O[C@@](O[C@@H](C)[C@@H]2OC(CC(C)C)=O)([H])C[C@]2(O)C)[C@@H]1N(C)C)([H])O[C@@H]([C@H](C[C@H]([C@H](/C=C/C=C/C3)O)C)CC=O)[C@H]([C@](CC(O[C@@H]3C)=O)([H])OC(C)=O)OC | ||
| 分子式 | C42H69NO15 | 分子量 | 827.99 |
| 溶解度 | DMSO : ≥ 41.67 mg/mL (50.33 mM);Water : 2 mg/mL (2.42 mM; ultrasonic and adjust pH to 3 with water) | 储存条件 | Store at 4°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 | 1.2077 mL | 6.0387 mL | 12.0774 mL |
| 5 mM | 0.2415 mL | 1.2077 mL | 2.4155 mL |
| 10 mM | 0.1208 mL | 0.6039 mL | 1.2077 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet