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Indolmycin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Indolmycin图片
CAS NO:21200-24-8
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Indolmycin (TAK-083) 是一种抗生素,是原核色氨酸-tRNA 连接酶 (TrpS) 的竞争性抑制剂。
Cas No.21200-24-8
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 SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.