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Lexithromycin (Erythromycin A 9-methoxime; Wy 48314) is a potent and semi-synthetic antibiotic derived from erythromycin A with antibacterial activity. It is prepared by reaction of the 9-keto moiety to methyl oxime. The structural change improves the pH stability profile and hydrophobicity of lexithromycin for better in vivo absorption. Thus lexithromycin has improved absorption in vivo over erythromycin due to increased hydrophopicity and pH stability. As with other macrolides, lexithromycin prevents protein synthesis by binding the ribosome at the polypeptide exit tunnel. Formulations containing lexithromycin were tested in clinical trials as treatment for HIV but were discontinued.
Targets |
Bacterial
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ln Vitro |
A derivative of erythromycin A, lexithromycin has antibacterial properties. For S. pyogenes CN10A and Streptococcus sp. 64/848C, lexithromycin exhibits a minimal inhibitory concentration (MIC) of 0.06 μg/mL; for Staphylococcus aureus Oxford, it is 0.25 μg/mL; for S. aureus Russell and S. aureus T2, it is 0.5 μg/mL; and for S. pyogenes CN10A and Haemophilus influenzae Wy 21[1].
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References |
Molecular Formula |
C38H70N2O13
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Molecular Weight |
762.968
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Exact Mass |
762.49
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Elemental Analysis |
C, 59.82; H, 9.25; N, 3.67; O, 27.26
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CAS # |
53066-26-5
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Appearance |
Solid powder
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SMILES |
CC[C@H]1OC([C@@H]([C@H]([C@@H]([C@H]([C@](O)(C[C@H](/C([C@@H]([C@H]([C@@]1(O)C)O)C)=N\OC)C)C)O[C@@H]2O[C@@H](C[C@H](N(C)C)[C@H]2O)C)C)O[C@H]3C[C@@](OC)([C@H]([C@@H](O3)C)O)C)C)=O
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InChi Key |
HPZGUSZNXKOMCQ-SQYJNGITSA-N
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InChi Code |
InChI=1S/C38H70N2O13/c1-15-26-38(10,46)31(42)21(4)28(39-48-14)19(2)17-36(8,45)33(53-35-29(41)25(40(11)12)16-20(3)49-35)22(5)30(23(6)34(44)51-26)52-27-18-37(9,47-13)32(43)24(7)50-27/h19-27,29-33,35,41-43,45-46H,15-18H2,1-14H3/b39-28+/t19-,20-,21+,22+,23-,24+,25+,26-,27+,29-,30+,31-,32+,33-,35+,36-,37-,38-/m1/s1
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Chemical Name |
(3R,4S,5S,6R,7R,9R,11S,12R,13S,14R,E)-6-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-14-ethyl-7,12,13-trihydroxy-4-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-10-(methoxyimino)-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
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Synonyms |
Lexithromycin; Wy-48314; Wy 48314; Wy48314;
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HS Tariff Code |
2934.99.03.00
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : ~50 mg/mL (~65.53 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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. Solubility in Formulation 2: ≥ 3.25 mg/mL (4.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. View More
Solubility in Formulation 3: ≥ 3.25 mg/mL (4.26 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+90% (20% SBE-β-CD in Saline): ≥ 5 mg/mL (6.55 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3107 mL | 6.5533 mL | 13.1067 mL | |
5 mM | 0.2621 mL | 1.3107 mL | 2.6213 mL | |
10 mM | 0.1311 mL | 0.6553 mL | 1.3107 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.