| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Macrolide antibiotic
Erythromycin glutamate targets the bacterial 50S ribosomal subunit. It binds to the 50S subunit and inhibits RNA-dependent protein synthesis by blocking transpeptidation. This prevents the elongation of the peptide chain, leading to bacteriostatic effects. It is metabolized through the liver and inhibits cytochrome enzyme P450 3A4. |
|---|---|
| ln Vitro |
Azithromycin, an azalide analog of erythromycin was assayed for its in vitro activity against multidrug-resistant Plasmodium falciparum K1 strain by measuring the 3H-hypoxanthine incorporation. Azithromycin caused inhibitory effects on the parasite growth with IC50 and IC90 values of 8.4+/-1.2 microM and 26.0+/-0.9 microM, respectively. 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[2].
In vitro, erythromycin glutamate is a potent and broad-spectrum antibiotic. It exhibits antibacterial activity against a wide range of Gram-positive and some Gram-negative bacteria. It is a macrolide bacteriostatic antibiotic. Minimum inhibitory concentrations (MICs) are determined by broth microdilution according to CLSI guidelines. |
| ln Vivo |
In vivo, erythromycin glutamate is used for the treatment of respiratory infections. It is a macrolide antibiotic with a broad spectrum of antibacterial activity. It is metabolized through the liver. Detailed pharmacokinetic data are available from clinical studies.
|
| Enzyme Assay |
Cell-free protein synthesis inhibition assays for erythromycin glutamate use bacterial ribosomes (70S) and a cell-free translation system. The compound is added at 0.1-100 µg/mL, and protein synthesis is measured by incorporation of radiolabeled amino acids (e.g., [3H]leucine) into acid-precipitable material. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
In vitro cellular assays for erythromycin glutamate use a panel of bacterial strains including Gram-positive (e.g., S. aureus, S. pneumoniae) and Gram-negative (e.g., H. influenzae). Minimum inhibitory concentrations (MICs) are determined by broth microdilution according to CLSI guidelines. Bacteria are cultured in appropriate media and treated with serial dilutions of erythromycin glutamate (0.1-100 µg/mL) for 18-24 hours, with MIC recorded as the lowest concentration showing no visible growth.
|
| Animal Protocol |
In vivo animal experiments for erythromycin glutamate use murine models of bacterial infection (e.g., pneumonia or sepsis). Erythromycin glutamate is administered orally or intravenously at doses of 1-50 mg/kg. Endpoints include survival, bacterial load in blood and tissues (CFU counts), and histopathological analysis of infected organs. Pharmacokinetic parameters are measured in plasma samples.
|
| References |
[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89. [3].\nBlood, tissue, and intracellular concentrations of erythromycin and its\nmetabolite anhydroerythromycin during and after therapy. Antimicrob\nAgents Chemother. 2012 Feb;56(2):1059-64. |
| Molecular Weight |
881.056040000001
|
|---|---|
| Exact Mass |
880.514
|
| Elemental Analysis |
C, 57.26; H, 8.69; N, 3.18; O, 30.87
|
| CAS # |
16667-03-1
|
| PubChem CID |
73456720
|
| Appearance |
Solid powder
|
| LogP |
1.749
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
61
|
| Complexity |
1320
|
| Defined Atom Stereocenter Count |
18
|
| SMILES |
OC(CC[C@H](N)C(O)=O)=O.CC[C@@H]1[C@](O)(C)[C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](O)(C)[C@H](O[C@H]2[C@H](O)[C@@H](N(C)C)C[C@@H](C)O2)[C@@H](C)[C@H](O[C@H]2C[C@](OC)(C)[C@@H](O)[C@H](C)O2)[C@@H](C)C(=O)O1
|
| InChi Key |
KNOXLRZTEFJWPE-OFWBJVIESA-N
|
| InChi Code |
InChI=1S/C37H67NO13.C5H9NO4/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)48-266-3(5(9)10)1-2-4(7)8/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H33H,1-2,6H2,(H,7,8)(H,9,10)/t18-,19-,20+,21+,22-,23+,24+,25?,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-3-/m10/s1
|
| Chemical Name |
(3R,4S,5S,6R,7R,9R,11R,12R,13S)-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
L-glutamate
|
| Synonyms |
Erythromycin glutamateHSDB 3074 HSDB-3074 HSDB3074 EmycinEryc-125 Eryc-250 Erythromycin
|
| HS Tariff Code |
2934.99.9001
|
| 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 | 1.1350 mL | 5.6750 mL | 11.3500 mL | |
| 5 mM | 0.2270 mL | 1.1350 mL | 2.2700 mL | |
| 10 mM | 0.1135 mL | 0.5675 mL | 1.1350 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
