Indolmycin
(Synonyms: 吲哚霉素,PA 155A,TAK-083) 目录号 : GC10766A selective inhibitor of bacterial tryptophanyl-tRNA synthetase
Cas No.:21200-24-8
Sample solution is provided at 25 µL, 10mM.
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IC50: 30 μM for prokaryotic tryptophanyl-tRNA synthetase
Indolmycin is an antibiotic.
Tryptophanyl-tRNA synthetase (TrpRS) catalyzes activation of tryptophan through ATP and transfer to tRNATrp , leading to translation of the genetic code for tryptophan.
In vitro: Indolmycin was found to ba a bacteriostatic that showed good activity against methicillin-resistant S. aureus, methicillin-susceptible Staphylococcus aureus, and vancomycin-intermediate S. aureus, including strains resistant to mupirocin or fusidic acid. Spontaneous indolmycin-resistant mutants was observed at a lower frequency than those selected by mupirocin or fusidic acid and exhibited no cross-resistance with the comparative drugs. High-level resistance of indolmycin at its MIC of 128 mg/L that was associated with an H43N mutation in tryptophanyl-tRNA synthetase, the target enzyme of indolmycin, led to loss of bacterial fitness. However, the locus responsible for low-level indolmycin resistance (indolmycin MICs 8-32 mg/L) was not identified [1].
In vivo: Animal study found that indolmycin could completely clear H. pylori in experimentally infected Mongolian gerbils at a dose of 10 mg/kg. Therefore, indolmycin could be regarded as a candidate for the treatment of H. pylori infection [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Hurdle JG, O'Neill AJ, Chopra I. Anti-staphylococcal activity of indolmycin, a potential topical agent for control of staphylococcal infections. J Antimicrob Chemother. 2004 Aug;54(2):549-52. Epub 2004 Jul 8.
[2] Vecchione JJ, Sello JK. A novel tryptophanyl-tRNA synthetase gene confers high-level resistance to indolmycin. Antimicrob Agents Chemother 2009; 53: 3972-3980.
| Cas No. | 21200-24-8 | SDF | |
| 别名 | 吲哚霉素,PA 155A,TAK-083 | ||
| 化学名 | 5S-[(1R)-1-(1H-indol-3-yl)ethyl]-2-(methylamino)-4(5H)-oxazolone | ||
| Canonical SMILES | O=C(N=C(NC)O1)[C@]1([H])[C@H](C)C2=CNC3=CC=CC=C32 | ||
| 分子式 | C14H15N3O2 | 分子量 | 257.3 |
| 溶解度 | Soluble in ethanol;methanol;DMSO;dimethyl formamide | 储存条件 | Store at -20°C, protect from light |
| 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 | 3.8865 mL | 19.4326 mL | 38.8651 mL |
| 5 mM | 0.7773 mL | 3.8865 mL | 7.773 mL |
| 10 mM | 0.3887 mL | 1.9433 mL | 3.8865 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: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet