Josamycin (EN-141) (Synonyms: Kitasamycin A3, Leucomycin A3, Turimycin A5) |
| Catalog No.GC32108 |
Josamycin (EN-141) (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 16846-24-5
Sample solution is provided at 25 µL, 10mM.
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Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.
Studies show that the average lifetime on the ribosome is 3 h for Josamycin and that the dissociation constants for Josamycin binding to the ribosome is 5.5 nM. Josamycin slows down formation of the first peptide bond of a nascent peptide in an amino acid-dependent way and completely inhibits formation of the second or third peptide bond, depending on peptide sequence at a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin. At a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin[1].
Blood and tissue levels of Josamycin after oral administration are 200 mg/kg to rabbits. Tissue levels are generally much higher than the blood levels, and 3 h after the administration, when the blood level is very low, the tissue levels are rather higher than those 1 h after the dose. One hour after the medication, the level in the lungs is the highest of all the tissue levels[2].
[1]. Lovmar M, et al. Kinetics of macrolide action: the Josamycin and erythromycin cases. J Biol Chem. 2004 Dec 17;279(51):53506-15. [2]. Osono T, et al. Pharmacokinetics of macrolides, lincosamides and streptogramins. J Antimicrob Chemother. 1985 Jul;16 Suppl A:151-66.
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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 | |
| Synonyms | Kitasamycin A3, Leucomycin A3, Turimycin A5 | ||
| 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 | ||
| Formula | C42H69NO15 | M.Wt | 827.99 |
| Solubility | DMSO : ≥ 41.67 mg/mL (50.33 mM);Water : 2 mg/mL (2.42 mM; ultrasonic and adjust pH to 3 with water) | Storage | Store at 4°C |
| 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 | 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 |
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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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