| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g |
Erythromycin lactobionate, the lactobionate salt of erythromycin, is a 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
|
|---|---|
| ln Vitro |
P. falciparum cannot grow in the presence of erythromycin lactobionate, having IC50 and IC90 values of 58.2 μM and 104.0 μM, respectively[1]. Erythromycin lactobionate (10 μM, 100 μM; 24 h, 72 h) exhibits anti-inflammatory and antioxidant properties. It also inhibits the accumulation of 4-HNE (p<0.01) and 8-OHdG (p<0.01) and considerably lowers the production of TNF-α (p<0.01) and Iba-1 (p<0.01)[4].
|
| ln Vivo |
Mice given a dose of 5 mg/kg of erythromycin lactobionate (gastric intubation; 0.1–50 mg/kg; 30-120 days) have longer survival times and less tumor growth[3]. Even 120 days after inoculation, mice protected by erythromycin lactobionate (gastric intubation; 5 mg/kg) survive; however, a 50 mg/kg dose shortens the mean survival time in tumor-bearing mice by 4-5 days[3]. In the rat model of cerebral ischemia reperfusion injury, erythromycin lactobionate (ih; single injection; 50 mg/kg) has a protective effect[4].
|
| Cell Assay |
Cell Viability Assay[4]
Cell Types: Embryos primary cortical neuron (from the cerebral cortices of 17-day-old Sprague-Dawley rat) Tested Concentrations: 10, 100 μM Incubation Duration: 24, 72 hrs (hours) Experimental Results: Improved the viability of cultured neuronal cells in vitro after 3 hrs (hours) oxygen-glucose deprivation (OGD). |
| Animal Protocol |
Animal/Disease Models: Female ddY mice (6 week-old) with EAC cells or CDF mice (6 week-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: diminished tumor growth and prolonged the mean survival time of mice from the dose of 5 mg/kg, however, the 50 mg/kg dosage shortened the MST in tumorbearing mice. Animal/Disease Models: Male SD (Sprague-Dawley) rats (8weeks old, 250-300 g)[4] Doses: 50 mg/kg Route of Administration: subcutaneous (sc) single injection Experimental Results: decreased infarct volume and edema volume, improved neurological deficit. |
| 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]. Hamada K, et al. Antitumor effect of erythromycin in mice. Chemotherapy. 1995 Jan-Feb. 41(1):59-69. [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. |
| Additional Infomation |
Erythromycin Lactobionate is the lactobionate salt form of erythromycin, a broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin lactobionate diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin lactobionate may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.
See also: Erythromycin (has active moiety). |
| Molecular Formula |
C49H89NO25
|
|---|---|
| Molecular Weight |
1092.22
|
| Exact Mass |
1091.572
|
| CAS # |
3847-29-8
|
| Related CAS # |
Erythromycin;114-07-8;Erythromycin stearate;643-22-1;Erythromycin (aspartate);30010-41-4
|
| PubChem CID |
71469
|
| Appearance |
Solid powder
|
| Density |
0.9083 (rough estimate)
|
| Boiling Point |
818.4ºC at 760mmHg
|
| Melting Point |
145-150°
|
| Flash Point |
448.8ºC
|
| Index of Refraction |
1.5300 (estimate)
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
26
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
75
|
| Complexity |
1580
|
| Defined Atom Stereocenter Count |
27
|
| 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)OC2CC(C)(C(C(C)O2)O)OC)OC3C(C(CC(C)O3)N(C)C)O)O)O)O.C([C@H](C([C@@H]([C@H](C(=O)O)O)O)OC1C(C(C(C(CO)O1)O)O)O)O)O
|
| InChi Key |
NNRXCKZMQLFUPL-WBMZRJHASA-N
|
| InChi Code |
InChI=1S/C37H67NO13.C12H22O12/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;13-1-3(15)10(7(18)8(19)11(21)22)24-12-9(20)6(17)5(16)4(2-14)23-12/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H3;3-10,12-20H,1-2H2,(H,21,22)/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-;3-,4-,5+,6+,7-,8-,9-,10-,12+/m11/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;(2R,3R,4R,5R)-2,3,5,6-tetrahydroxy-4-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyhexanoic acid
|
| 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) |
DMSO: > 10 mM
|
|---|---|
| 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 | 0.9156 mL | 4.5778 mL | 9.1557 mL | |
| 5 mM | 0.1831 mL | 0.9156 mL | 1.8311 mL | |
| 10 mM | 0.0916 mL | 0.4578 mL | 0.9156 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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