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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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Purity: ≥98%
Dirithromycin (also known as LY-237216) is an Erythromycin derivative acting as a potent and orally bioactive semi-synthetic macrolide glycopeptide antibiotic, working by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides. Dirithromycin is a more lipid-soluble prodrug derivative of 9S-erythromycyclamine prepared by condensation of the latter with 2-(2-methoxyethoxy)acetaldehyde. The 9N, 11O-oxazine ring thus formed is a hemi-aminal that is unstable under both acidic and alkaline aqueous conditions and undergoes spontaneous hydrolysis to form erythromycyclamine.
Targets |
Macrolide
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ln Vitro |
Similar to erythromycin, dirithromycin has an antimicrobial activity spectrum in vitro.
With MICs of approximately 1.0 and <0.25 μg/mL at pH values of 7.1 and 7.4, respectively, dirithromycin demonstrates good in vitro activity against a number of strains of Legionella.
With MICs of less than 0.5 μg/mL, dirithromycin exhibits strong activity against a number of Helicobacter pytori strains[2].
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ln Vivo |
With ED50s of 1.0, 0.6, and <0.6 mg/kg, dirithromycin (s.c. for two times) is effective against experimental infections in mice caused by S. aureus, S. pyogenes, and S. pneumoniae[2].
With ED50s of 27, 34, and 23 mg/kg, respectively, dirithromycin (p.o. for two times) is effective against experimental infections in mice caused by S. aureus, S. pyogenes, and S. pneumoniae[2]. |
References |
Molecular Formula |
C42H78N2O14
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Molecular Weight |
835.0737
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Exact Mass |
834.55
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Elemental Analysis |
C, 60.41; H, 9.42; N, 3.35; O, 26.82
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CAS # |
62013-04-1
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Appearance |
Solid powder
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SMILES |
CC[C@@H]1[C@](O)(C)[C@@]2([H])[C@@H](C)[C@](N[C@@H](COCCOC)O2)([H])[C@H](C)C[C@@](C)(O)[C@@](O[C@]3([H])O[C@H](C)C[C@H](N(C)C)[C@H]3O)([H])[C@@H](C)[C@H](O[C@]4([H])O[C@@H](C)[C@H](O)[C@@](OC)(C)C4)[C@@H]
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InChi Key |
WLOHNSSYAXHWNR-DWIOZXRMSA-N
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InChi Code |
InChI=1S/C42H78N2O14/c1-15-29-42(10,49)37-24(4)32(43-30(56-37)21-52-17-16-50-13)22(2)19-40(8,48)36(58-39-33(45)28(44(11)12)18-23(3)53-39)25(5)34(26(6)38(47)55-29)57-31-20-41(9,51-14)35(46)27(7)54-31/h22-37,39,43,45-46,48-49H,15-21H2,1-14H3/t22-,23-,24+,25+,26-,27+,28+,29-,30-,31+,32+,33-,34+,35+,36-,37-,39+,40-,41-,42-/m1/s1
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Chemical Name |
(1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-9-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-3-ethyl-2,10-dihydroxy-7-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-15-((2-methoxyethoxy)methyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one
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Synonyms |
LY237216; LY 237216; LY-237216;Antibiotic AS-E 136;
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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 |
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) |
Ethanol : 100~50 mg/mL(59.88 mM)
DMSO : 11~33.33 mg/mL ( 13.17~39.91 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.99 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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 (2.99 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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 (2.99 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% EtOH+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (2.99 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.1975 mL | 5.9875 mL | 11.9750 mL | |
5 mM | 0.2395 mL | 1.1975 mL | 2.3950 mL | |
10 mM | 0.1198 mL | 0.5988 mL | 1.1975 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.