| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Josamycin (BRN-1677122; CCRIS 8511; EN-141) is a macrolide antibiotic that exhibits antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM. It is synthesized from strains of Streptomyces narbonensis var.
| Targets |
Macrolide
|
|---|---|
| ln Vitro |
According to studies, josamycin has an average lifetime of 3 hours on the ribosome and a dissociation constant of 5.5 nM when it binds to the ribosome. Josamycin completely prevents the synthesis of full-length proteins at saturating drug concentrations by completely inhibiting the formation of the second or third peptide bond, depending on the peptide sequence. Josamycin also slows down the formation of the first peptide bond of a nascent peptide in an amino acid-dependent manner. Josamycin completely inhibits the synthesis of full-length proteins at a saturating drug concentration[1].
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| ln Vivo |
After giving rabbits 200 mg/kg of josamycin orally, the drug is present in their blood and tissues. In general, tissue levels are significantly higher than blood levels, and they are also somewhat higher three hours after the dose than they are one hour later, when the blood level is at its lowest. The level in the lungs is the highest of all tissue levels one hour after the medication[2].
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| Enzyme Assay |
0.5 mM calcium chloride, 5 mM magnesium acetate, 5 mM ammonium chloride, 95 mM potassium chloride, 8 mM putrescine, 1 mM spermidine, 5 mM potassium phosphate, and 1 mM dithioerythritol are the ingredients used to prepare josamycin in polymix buffer. Preinitiated ribosomes are treated with varying concentrations of josamycin (2, 3, 4, and 6 μM) to initiate the incubation process. At each incubation period, one volume of the reaction mix is mixed with one volume of the elongation mix. The reaction is then quenched with formic acid after ten seconds. The fraction of ribosomes that form tripeptides is used to estimate the association rates[1].
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| Animal Protocol |
Rat: Rats are given 200 mg/kg of oral Josamycin labeled with tritium. Bioassay is used to determine the blood and tissue levels at one hour and three hours[2].
Mouse: Mice are given 200 mg/kg of josamycin labeled with tritium orally. Bioassay is used to determine the blood and tissue levels at one hour and three hours[2]. |
| References |
| Molecular Formula |
C42H69NO15
|
|---|---|
| Molecular Weight |
827.99496
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| Exact Mass |
827.47
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| Elemental Analysis |
C, 60.92; H, 8.40; N, 1.69; O, 28.98
|
| CAS # |
16846-24-5
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| Related CAS # |
31674-19-8 (Josamycin propionate); 11033-19-5 (Josamycin HCl); 4564-87-8 (Carbomycin); 35775-82-7 (Maridomycin); 20283-69-6 (niddamycin); 1404-48-4 (relomycin);35834-26-5 (rosaramicin); 497-72-3 (methymycin); 30042-37-6 (lankamycin )
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| Appearance |
Solid powder
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| SMILES |
O([C@@H]1[C@H]([C@@H](CC(O[C@@H](CC=CC=C[C@@H]([C@@H](C[C@@H]1CC=O)C)O)C)=O)OC(C)=O)OC)[C@H]1[C@@H]([C@H]([C@H](O[C@H]2C[C@@]([C@@H](OC(CC(C)C)=O)[C@@H](O2)C)(C)O)[C@H](O1)C)N(C)C)O
|
| InChi Key |
XJSFLOJWULLJQS-DJBGMQKKSA-N
|
| InChi Code |
InChI=1S/C42H69NO15/c1-23(2)19-32(47)56-40-27(6)53-34(22-42(40,8)50)57-37-26(5)54-41(36(49)35(37)43(9)10)58-38-29(17-18-44)20-24(3)30(46)16-14-12-13-15-25(4)52-33(48)21-31(39(38)51-11)55-28(7)45/h12-14,16,18,23-27,29-31,34-41,46,49-50H,15,17,19-22H2,1-11H3/b13-12-,16-14+/t24-,25-,26-,27+,29+,30+,31-,34+,35-,36-,37-,38+,39+,40+,41+,42-/m1/s1
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| Chemical Name |
Leucomycin V, 3-acetate 4(sup B)-(3-methylbutanoate)
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| Synonyms |
Josamycin; BRN-1677122; CCRIS 8511; BRN 1677122; BRN1677122; Josamycin hydrochloride; Leucomycin A3 hydrochloride;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 41.67~100 mg/mL (50.33~120.77 mM)
H2O : 8.33 mg/mL (10.06 mM) Ethanol : ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.02 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (3.02 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (3.02 mM) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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