Erythromycin estolate
Based on 1 publication(s) in Google Scholar
Erythromycin estolate is the Erythromycin (HY-B0220) derivative, is a macrolide antibiotic used in the treatment of a wide variety of bacterial infections. Erythromycin estolate causes several cases of liver injury which mostly include cholestatic hepatitis. Erythromycin estolate toxicity is related to its inhibitory effect on bile acid transport.
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- Reinheit: 98.0%
- CAS. Nr.: 3521-62-8
- Formel: C52H97NO18S
- Molecular Weight:1056.39
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Erythromycin estolate
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
11.4 μM
Compound: Erythromycin estolate
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
4.1 μM
Compound: Erythromycin estolate
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
Erythromycin estolate inactivates viral particles by destroying the integrity of the viral membrane, resulting in the release of viral genomic RNA, and the irreversible loss of infection ability. Erythromycin estolate inhibits various flaviviruses, including Zika virus (ZIKV), dengue virus (DENV), yellow fever virus (YFV) and human coronavirus OC43 (HCoV-OC43)[2].
Erythromycin estolate (2.5-10 µM, 48 h) reduces the virus titer of HCoV-OC43 with an IC50 of 1.40 µM, reduces the number of HCoV-OC43 infected BHK-21 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BHK-21
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Concentration:2.5-10 µM
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Incubation Time:48 h
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Result:Reduced the viral nucleoprotein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats models[1]
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Dosage:450-1200 mg/kg
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Administration:po, once daily for 7 days
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Result:Caused hydropic degeneration of hepatocytes.
Increased serum bilirubin (TBILI) levels and alanine aminotransferase (ALT) activity.
Decreased serum triglyceride (TG) levels and glutathione (GSH) content in liver tissue.
Chemical Information
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CAS. Nr. 3521-62-8
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Appearance Solid
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Molecular Weight 1056.39
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Formel C52H97NO18S
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Color White to off-white
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SMILES
CCCCCCCCCCCCOS(=O)(O)=O.CCC(O[C@H]([C@H](C[C@@H](C)O1)N(C)C)[C@]1([H])O[C@@H]2[C@H]([C@@H]([C@H](C(O[C@@H]([C@@](C)(O)[C@H](O)[C@@H](C)C([C@H](C)C[C@]2(O)C)=O)CC)=O)C)O[C@@]3([H])C[C@](C)([C@@H](O)[C@H](C)O3)OC)C)=O
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Initial Source
Streptomyces erythrus
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Viruses
Erythromycin Estolate Inhibits Zika Virus Infection by Blocking Viral Entry as a Viral Inactivator. [Abstract]2019 Nov 15;11(11):1064. PMID: 31731598
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (94.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (1.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lu X, et al. Integrated systems toxicology approaches identified the possible involvement of ABC transporters pathway in erythromycin estolate-induced liver injury in rat. Food Chem Toxicol. 2014 Mar;65:343-55. [Content Brief]
[2]. Wang X, et al., Erythromycin Estolate Is a Potent Inhibitor Against HCoV-OC43 by Directly Inactivating the Virus Particle. Front Cell Infect Microbiol. 2022 Jul 7;12:905248. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9466 mL | 4.7331 mL | 9.4662 mL | 23.6655 mL |
| 5 mM | 0.1893 mL | 0.9466 mL | 1.8932 mL | 4.7331 mL | |
| 10 mM | 0.0947 mL | 0.4733 mL | 0.9466 mL | 2.3666 mL | |
| 15 mM | 0.0631 mL | 0.3155 mL | 0.6311 mL | 1.5777 mL | |
| 20 mM | 0.0473 mL | 0.2367 mL | 0.4733 mL | 1.1833 mL | |
| 25 mM | 0.0379 mL | 0.1893 mL | 0.3786 mL | 0.9466 mL | |
| 30 mM | 0.0316 mL | 0.1578 mL | 0.3155 mL | 0.7889 mL | |
| 40 mM | 0.0237 mL | 0.1183 mL | 0.2367 mL | 0.5916 mL | |
| 50 mM | 0.0189 mL | 0.0947 mL | 0.1893 mL | 0.4733 mL | |
| 60 mM | 0.0158 mL | 0.0789 mL | 0.1578 mL | 0.3944 mL | |
| 80 mM | 0.0118 mL | 0.0592 mL | 0.1183 mL | 0.2958 mL |
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