Indolmycin (Synonyms: PA 155A,TAK-083) |
Catalog No.GC10766
One-Click Copy Product Info
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L'indolmycine (TAK-083), un antibiotique, est un inhibiteur compétitif de la tryptophanyl-tRNA ligase procaryote (TrpS).
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonymes | PA 155A,TAK-083 | ||
| Chemical Name | 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 | ||
| Formula | C14H15N3O2 | M.Wt | 257.3 |
| Solubility | Soluble in ethanol;methanol;DMSO;dimethyl formamide | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8865 mL | 19.4326 mL | 38.8651 mL |
| 5 mM | 777.3 μL | 3.8865 mL | 7.773 mL |
| 10 mM | 388.7 μL | 1.9433 mL | 3.8865 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)