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Erythromycin estolate

Name: Erythromycin estolate
Brand: TargetMol
SKU: T15245
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15245Cas No. 3521-62-8

Alias Phtalic anhydride, ilosone

Erythromycin estolate is a semi-synthetic derivative of erythromycin with good oral absorption and bioavailability tolerance. As a macrolide antibiotic, Erythromycin exerts its antibacterial action by inhibiting bacterial protein synthesis and is mainly used in studies for the treatment of respiratory, skin and soft tissue infections caused by susceptible bacteria. Erythromycin estolate may cause liver injury, including mild cholestatic hepatitis, jaundice, and paucity of bile ducts.

Erythromycin estolate

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Purity: 99.59%

Catalog No. T15245Alias Phtalic anhydride, ilosoneCas No. 3521-62-8

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$33	In Stock	In Stock
100 mg	$48	In Stock	In Stock
500 mg	$119	In Stock	In Stock
1 g	$175	-	In Stock
1 mL x 10 mM (in DMSO)	$37	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.59%

Potency:600 μg/mg dry weight

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Erythromycin estolate AI Summary

Erythromycin estolate exhibits inhibitory activity on the uptake of sodium fluorescein in OATP1B3-transfected CHO cells, with a 7.433% inhibition at 10 µM concentration, an IC50 value of 3090.3 nM, and a Ki value of 2350.0 nM. Similarly, in OATP1B1-transfected CHO cells, it shows a 6.903% inhibition at the same concentration, an IC50 value of 4365.16 nM, and a Ki value of 2410.0 nM. The compound also inhibits the uptake of [3H]taurocholate in both Sprague-Dawley rat and human BSEP expressed in plasma membrane vesicles, with IC50 values of 11400.0 nM and 4100.0 nM, respectively. Furthermore, it inhibits human BSEP with an IC50 value of 13000.0 nM, causing a reduction in ATP-dependent taurocholate uptake and demonstrating the inhibition of vesicle-associated [3H]-taurocholate transport. The compound induces mitochondrial dysfunction in rat liver mitochondria by inhibiting mitochondrial respiration and has a Cmax value of 4196.0 nM in humans when administered as a single dose. In the context of antiviral activity, Erythromycin estolate inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, showing 4.1% and 0.48% inhibition respectively at a 10 µM concentration after 48 hours exposure. Additionally, it inhibits the SARS-CoV-2 3CL-Pro protease by 20.05% at a concentration of 20 µM, indicating potential antiviral properties against SARS-CoV-2..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Erythromycin estolate is a semi-synthetic derivative of erythromycin with good oral absorption and bioavailability tolerance. As a macrolide antibiotic, Erythromycin exerts its antibacterial action by inhibiting bacterial protein synthesis and is mainly used in studies for the treatment of respiratory, skin and soft tissue infections caused by susceptible bacteria. Erythromycin estolate may cause liver injury, including mild cholestatic hepatitis, jaundice, and paucity of bile ducts.
In vitro	Erythromycin estolate effectively inhibited HCoV-OC43 infection in different cell types and significantly reduced virus titers at safe concentration without cell cytotoxicity. Furthermore, erythromycin estolate was identified to inhibit HCoV-OC43 infection at the early stage and to irreversibly inactivate virus by disrupting the integrity of the viral membrane whose lipid component might be the target of action. Together, it was demonstrated that erythromycin estolate could be a potential therapeutic drug for HCoV-OC43 infection.[1]
Synonyms	Phtalic anhydride, ilosone

Chemical Properties

Molecular Weight	1056.39
Formula	C₅₂H₉₇NO₁₈S
Cas No.	3521-62-8
Smiles	CCCCCCCCCCCCOS(O)(=O)=O.CCC1OC(=O)C(C)C(OC2CC(C)(OC)C(O)C(C)O2)C(C)C(OC2OC(C)CC(C2OC(=O)CC)N(C)C)C(C)(O)CC(C)C(=O)C(C)C(O)C1(C)O
Relative Density.	1.0053 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (42.6 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (1.89 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.9466 mL	4.7331 mL	9.4662 mL	47.3310 mL
5 mM	0.1893 mL	0.9466 mL	1.8932 mL	9.4662 mL
10 mM	0.0947 mL	0.4733 mL	0.9466 mL	4.7331 mL
20 mM	0.0473 mL	0.2367 mL	0.4733 mL	2.3666 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc