| Size | Price | |
|---|---|---|
| 1g | ||
| 2g | ||
| 5g | ||
| 10g | ||
| 25g |
Description: Erythromycin stearate, the stearate salt of Erythromycin, is a macrolide antibiotic isolated from actinomycete Streptomyces erythreus, acting by binding to bacterial 50S ribosomal subunits and inhibiting RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid. It exhibits a broad spectrum of antimicrobial activity as well as antitumor and neuroprotective effects.
| Targets |
Macrolide antibiotic
|
|---|---|
| ln Vitro |
Plasmodium falciparum cannot develop in the presence of erythromycin stearate, which has IC50 and IC90 values of 58.2 μM and 104.0 μM, respectively [1]. In addition to its anti-inflammatory and antioxidant properties, erythromycin stearate (10 μM, 100 μM; 24 hours, 72 hours) also dramatically lowers the expression of TNF-α (p<0.01) and Iba-1 (p<0.01) and prevents the formation of 4-HNE (p<0.01) and 8-OHdG (p<0.01) [4].
|
| ln Vivo |
Erythromycin stearate (gastric intubation; 0.1-50 mg/kg; 30-120 days) decreases tumor growth and prolongs survival in mice at a dose of 5 mg/kg [3]. Erythromycin stearate (gastric intubation; 5 mg/kg) maintained mouse survival even at 120 days postinoculation, whereas a dose of 50 mg/kg decreased the mean survival period of tumor-bearing mice by 4- 5 days[3]. Erythromycin stearate (ih; single injection; 50 mg/kg) has a protective effect on brain ischemia-reperfusion injury rat model [4].
|
| Cell Assay |
Cell viability assay [4]
Cell Types: Embryonic primary cortical neurons (from the cerebral cortex of 17-day-old Sprague-Dawley rats) Tested Concentrations: 10, 100 μM Incubation Duration: 24, 72 hrs (hours) Experimental Results: Improved viability of cultured neurons 3 hrs (hours) of oxygen-glucose deprivation (OGD) in vitro cells. |
| Animal Protocol |
Animal/Disease Models: Female ddY mice (6 weeks old) with EAC cells or CDF mice (6 weeks old) with P388 cells [3]
Doses: 0.1 mg/kg; 0.5 mg/kg; 10 mg/kg ; 30 mg/kg; 50 mg/kg Route of Administration: gastric intubation; 30-120 days Experimental Results: After the 5 mg/kg dose, tumor growth was diminished and the average survival time of mice was prolonged, but the 50 mg/kg dose shortened the load. MST of tumor mice. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (8 weeks old, 250-300 g) [4] Doses: 50 mg/kg Route of Administration: Single subcutaneous injection Experimental Results: Reduce infarct volume and edema volume, and improve neurological deficits. |
| References |
[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89.
[2]. Nakornchai S, et al. Activity of azithromycin or erythromycin in combination with antimalarial drugs against multidrug-resistant Plasmodium falciparum in vitro. Acta Trop. 2006 Dec;100(3):185-91. Epub 2006 Nov 28. [3]. K Hamada, et al. Antitumor Effect of Erythromycin in Mice. Chemotherapy [4]. Katayama Y, et al. Neuroprotective effects of erythromycin on cerebral ischemia reperfusion-injury and cell viability after oxygen-glucose deprivation in cultured neuronal cells. Brain Res. 2014 Nov 7. 1588:159-67. |
| Molecular Formula |
C55H103NO15
|
|---|---|
| Molecular Weight |
1018.40
|
| Exact Mass |
1003.7171
|
| CAS # |
643-22-1
|
| Related CAS # |
Erythromycin;114-07-8;Erythromycin lactobionate;3847-29-8;Erythromycin (aspartate);30010-41-4;Erythromycin thiocyanate;7704-67-8;Erythromycin A dihydrate;59319-72-1
|
| Appearance |
Solid
|
| LogP |
8.1
|
| tPSA |
231.210
|
| SMILES |
CC[C@@H]1[C@](C)([C@@H]([C@@H](C)C(=O)[C@H](C)C[C@](C)([C@@H]([C@@H](C)[C@@H]([C@@H](C)C(=O)O1)O[C@H]2C[C@](C)([C@H]([C@H](C)O2)O)OC)O[C@H]3[C@@H]([C@H](C[C@@H](C)O3)N(C)C)O)O)O)O.CCCCCCCCCCCCCCCCCC(=O)O
|
| InChi Key |
YAVZHCFFUATPRK-YZPBMOCRSA-N
|
| InChi Code |
InChI=1S/C37H67NO13.C18H36O2/c1-14-25-37(10,45)30(41)20(4)27(39)18(2)16-35(8,44)32(51-34-28(40)24(38(11)12)15-19(3)47-34)21(5)29(22(6)33(43)49-25)50-26-17-36(9,46-13)31(42)23(7)48-26;1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18(19)20/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H3;2-17H2,1H3,(H,19,20)/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-;/m1./s1
|
| Chemical Name |
(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione;octadecanoic acid
|
| HS Tariff Code |
2942000000
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9819 mL | 4.9097 mL | 9.8193 mL | |
| 5 mM | 0.1964 mL | 0.9819 mL | 1.9639 mL | |
| 10 mM | 0.0982 mL | 0.4910 mL | 0.9819 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.
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