| Size | Price | Stock | Qty |
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| 25g |
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Purity: ≥98%
Erythromycin is a potent and broad-spectrum antibiotic belonging to a group of drugs called macrolide antibiotics, it is produced by actinomycete Streptomyces erythreus and is an inhibitor of protein translation and mammalian mRNA splicing. It acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid, thus inhibiting growth of gram negative and gram positiove bacteria. Erythromycin is used to treat certain infections caused by bacteria, such as infections of the respiratory tract, including bronchitis, pneumonia, Legionnaires' disease (a type of lung infection), and pertussis (whooping cough; a serious infection that can cause severe coughing); diphtheria (a serious infection in the throat); sexually transmitted diseases (STD), including syphilis; and ear, intestine, gynecological, urinary tract, and skin infections.
| Targets |
Macrolide antibiotic
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|---|---|
| ln Vitro |
P. falciparum cannot grow when erythromycin is present; its IC50 and IC90 values are 58.2 μM and 104.0 μM, respectively[1].
Erythromycin (10 μM, 100 μM; 24 h, 72 h) exhibits anti-inflammatory and antioxidant properties. It also suppresses the accumulation of 4-HNE (p<0.01) and 8-OHdG (p<0.01) and significantly lowers the expression of TNF-α (p<0.01) and Iba-1 (p<0.01)[4]. |
| ln Vivo |
Erythromycin (gastric intubation; 0.1–50 mg/kg; 30-120 days) slows the growth of tumors and increases the amount of time that mice survive after receiving a dose of 5 mg/kg.When given at a dose of 50 mg/kg, erythromycin (gastric intubation; 5 mg/kg) shortens the mean survival time in tumor-bearing mice by 4-5 days. However, it protects mice alive even 120 days after inoculation.[3].
A single injection of erythromycin (i.h.; 50 mg/kg) protects against cerebral ischemia reperfusion injury in a rat model[4].
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| Enzyme Assay |
Erythromycin inhibited growth of P. falciparum with IC50 and IC90 values of 58.2+/-7.7 microM and 104.0+/-10.8 microM, respectively. The activity of antimalarial drugs in combination with azithromycin or erythromycin against P. falciparum K1 were compared. Combinations of chloroquine with azithromycin or erythromycin showed synergistic effects against parasite growth in vitro. Combinations of quinine-azithromycin and quinine-erythromycin showed potentiation. Additive effects were observed in mefloquine-azithromycin and mefloquine-erythromycin combinations. Similar results were also produced by pyronaridine in combination with azithromycin or erythromycin. However, artesunate-azithromycin and artesunate-erythromycin combinations had antagonistic effects. The in vitro data suggest that azithromycin and erythromycin will have clinical utility in combination with chloroquine and quinine. The worldwide spread of chloroquine-resistant P. falciparum might inhibit the ability to treat malaria patients with chloroquine-azithromycin and chloroquine-erythromycin in areas of drug-resistant. The best drug combinations against multidrug-resistant P. falciparum are quinine-azithromycin and quinine-erythromycin [4].
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| Cell Assay |
Cell Line: Primary cortical neuron of embryos (derived from the cerebral cortices of Sprague-Dawley rats 17 days old)
Concentration: 10, 100 μM Incubation Time: 24, 72 hours Result: increased the cultivated neuronal cells' viability in vitro following three hours of oxygen-glucose deprivation (OGD). |
| Animal Protocol |
Animal Model: Six-week-old female ddY mice with EAC cellsor six-week-old CDF mice with P388 cells[3]
Dosage: 0.1 mg/kg; 0.5 mg/kg; 10 mg/kg; 30 mg/kg; 50 mg/kg
Administration: Gastric intubation; 30-120 days
Result: reduced tumor growth and extended the mice's mean survival time (5 mg/kg); in contrast, the 50 mg/kg dose caused the MST in tumor-bearing mice to be shorter.
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| References |
| Molecular Formula |
C37H67NO13
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|---|---|
| Molecular Weight |
733.9268
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| Exact Mass |
733.46
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| Elemental Analysis |
C, 60.55; H, 9.20; N, 1.91; O, 28.34
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| CAS # |
114-07-8
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| Related CAS # |
Erythromycin-d6;959119-25-6;Erythromycin-d3;959119-26-7;Erythromycin Ethylsuccinate;1264-62-6;Erythromycin stearate;643-22-1;Erythromycin lactobionate;3847-29-8;Erythromycin (aspartate);30010-41-4;Erythromycin thiocyanate;7704-67-8;Erythromycin A dihydrate;59319-72-1;Erythromycin-13C,d3;2378755-50-9
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| Appearance |
White to off-white solid powder
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| Source |
Streptomyces erythreHs
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| LogP |
2.83
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| tPSA |
193.91
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| SMILES |
C[C@@H]([C@@H]([C@H](C(O[C@@H]([C@@]([C@H](O)[C@@H](C)C1=O)(C)O)CC)=O)C)O[C@H]2C[C@]([C@@H](O)[C@H](C)O2)(OC)C)[C@H]([C@](C)(O)C[C@H]1C)O[C@H](O[C@@H](C[C@@H]3N(C)C)C)[C@@H]3O
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| InChi Key |
ULGZDMOVFRHVEP-RWJQBGPGSA-N
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| InChi Code |
InChI=1S/C37H67NO13/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/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H3/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-/m1/s1
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| Chemical Name |
(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-14-ethyl-7,12,13-trihydroxy-4-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione
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| Synonyms |
Emycin; HSDB 3074; HSDB-3074; HSDB3074; Eryc-125; Eryc-250; Erythromycin
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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) |
DMSO : ≥ 100 mg/mL (136.25 mM)
Ethanol : ~100 mg/mL H2O : 1 mg/mL (1.36 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 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 20.8 mg/mL clear DMSO 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: ≥ 2.08 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 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 20.8 mg/mL clear DMSO 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: ≥ 2.08 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (2.83 mM) Solubility in Formulation 5: 5 mg/mL (6.81 mM) in 0.5% CMC-Na 0.1% Tween-80 (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3625 mL | 6.8126 mL | 13.6253 mL | |
| 5 mM | 0.2725 mL | 1.3625 mL | 2.7251 mL | |
| 10 mM | 0.1363 mL | 0.6813 mL | 1.3625 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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