Dirithromycin
Based on 1 publication(s) in Google Scholar
Dirithromycin (LY237216), a derivative of Erythromycin, is a potent and orally active semi-synthetic macrolide antibiotic. Dirithromycin is active against gram-positive bacteria, Legionella spp., Helicobacter pylori, and Chlamydia trachomatis.
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- Pureté: 98.0%
- CAS No.: 62013-04-1
- Formule: C42H78N2O14
- Masse moléculaire:835.07
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Dirithromycin
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Activité biologique
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Macrolide |
Dirithromycin possesses an in vitro spectrum of antimicrobial activity which is similar to that of Erythromycin[2].
Dirithromycin exhibits excellent in vitro activity against several strains of Legionella, with MICs of ~1.0 and <0.25 μg/mL at pH=7.1 and 7.4, respectively[2].
Dirithromycin demonstrates potent activity against several strains of Helicobacter pytori, with MICs of <0.5 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Dirithromycin (p.o. for 2 times) is effective against experimental infections caused by S. aureus, S. pyogenes, and S. pneumoniae in mice, with ED50s of 27, 34, and 23 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 62013-04-1
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Appearance Solid
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Masse moléculaire 835.07
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Formule C42H78N2O14
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Color White to off-white
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SMILES
CC1[C@@]([C@](O)([C@H](OC([C@@H]2C)=O)CC)C)([H])O[C@H](COCCOC)N[C@@]1([H])[C@](C[C@@](O)([C@@H]([C@@H](C)[C@]2([H])O[C@@](O[C@@H](C)[C@@H]3O)([H])C[C@@]3(C)OC)O[C@@](O[C@H](C)C[C@@H]4N(C)C)([H])[C@@H]4O)C)([H])C
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Synonyms
LY237216
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Prolif
Direct inhibitory effect on viral entry of influenza A and SARS-CoV-2 viruses by azithromycin. [Abstract]2021 Jan;54(1):e12953. PMID: 33211371
Solvant et solubilité
Ethanol : ≥ 50 mg/mL (59.88 mM)
DMSO : 33.33 mg/mL (39.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Wasilewski MM, et, al. Five-day dirithromycin therapy is as effective as seven-day erythromycin therapy for acute exacerbations of chronic bronchitis. J Antimicrob Chemother. 1999 Apr;43(4):541-8. [Content Brief]
[2]. Counter FT, et, al. Synthesis and antimicrobial evaluation of dirithromycin (AS-E 136; LY237216), a new macrolide antibiotic derived from erythromycin. Antimicrob Agents Chemother. 1991 Jun;35(6):1116-26. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 1.1975 mL | 5.9875 mL | 11.9750 mL | 29.9376 mL |
| 5 mM | 0.2395 mL | 1.1975 mL | 2.3950 mL | 5.9875 mL | |
| 10 mM | 0.1198 mL | 0.5988 mL | 1.1975 mL | 2.9938 mL | |
| 15 mM | 0.0798 mL | 0.3992 mL | 0.7983 mL | 1.9958 mL | |
| 20 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4969 mL | |
| 25 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1975 mL | |
| 30 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9979 mL | |
| Ethanol | 40 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7484 mL |
| 50 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL |