1. Anti-infection
  2. Bacterial

Josamycin (Synonyms: EN-141)

Cat. No.: HY-B1920 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Josamycin Chemical Structure

Josamycin Chemical Structure

CAS No. : 16846-24-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
25 mg USD 50 In-stock
Estimated Time of Arrival: December 31
100 mg USD 140 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

Kd: 5.5 nM (ribosome)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : 2 mg/mL (2.42 mM; ultrasonic and adjust pH to 3 with 水)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

827.99

Formula

C₄₂H₆₉NO₁₅

CAS No.

16846-24-5

SMILES

O[[email protected]]1[[email protected]](O[[email protected]](C)[[email protected]@H](O[[email protected]@](O[[email protected]@H](C)[[email protected]@H]2OC(CC(C)C)=O)([H])C[[email protected]]2(O)C)[[email protected]@H]1N(C)C)([H])O[[email protected]@H]([[email protected]](C[[email protected]]([[email protected]](/C=C/C=C/C3)O)C)CC=O)[[email protected]]([[email protected]](CC(O[[email protected]@H]3C)=O)([H])OC(C)=O)OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Josamycin
Cat. No.:
HY-B1920
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Josamycin

Cat. No.: HY-B1920