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Erythromycin thiocyanate 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 |
Plasmodium falciparum is inhibited by erythromycin thiocyanate, with IC50 and IC90 values of 58.2 μM and 104.0 μM, respectively [1]. Antioxidant and anti-inflammatory properties of erythromycin thiocyanate (10 μM, 100 μM; 24 hours, 72 hours) include inhibiting the formation of 4-HNE (p<0.01) and 8-OHdG (p<0.01), reducing Iba-1 (p<0.01), and dramatically reducing TNF-α (p<0.01) [4].
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| ln Vivo |
Mice given erythromycin thiocyanate (0.1–50 mg/kg; 30-120 days) at a dose of 5 mg/kg have tumor growth inhibition and longer survival times [3]. Even 120 days after injection, mice protected against tumor growth by erythromycin thiocyanate (gastric intubation; 5 mg/kg); however, a 50 mg/kg dose reduced the average life period of tumor-bearing mice by 4–5 days[3]. In a rat model of cerebral ischemia-reperfusion injury, erythromycin thiocyanate (ih; single injection; 50 mg/kg) exhibits a protective effect [4].
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| 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]. 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. |
| Molecular Formula |
C₃₈H₆₈N₂O₁₃S
|
|---|---|
| Molecular Weight |
793.02
|
| Exact Mass |
791.4369
|
| CAS # |
7704-67-8
|
| Related CAS # |
Erythromycin;114-07-8;Erythromycin stearate;643-22-1
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.18
|
| tPSA |
256.50
|
| SMILES |
C[C@@H]([C@@H]([](C(O[C@@H]1CC)=O)C)O[C@@](O[C@@H](C)[C@@H]2O)([H])C[C@@]2(C)OC)[]([C@](O)(C[](C([C@@H]([C@@H](O)[C@@]1(O)C)C)=O)C)C)O[C@@](O[](C)C[C@@H]3N(C)C)([H])[C@@H]3O.SC#N
|
| InChi Key |
WVRRTEYLDPNZHR-YZPBMOCRSA-N
|
| InChi Code |
InChI=1S/C37H67NO13.CHNS/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;2-1-3/h18-26,28-32,34,40-42,44-45H,14-17H2,1-13H3;3H/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;thiocyanic acid
|
| Synonyms |
Erythromycin thiocyanate; Erythromycin (thiocyanate); Erythromycin, thiocyanate (salt); UNII-Y7A95YRI88
|
| HS Tariff Code |
2941500000
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~126.10 mM)
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|---|---|
| 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 | 1.2610 mL | 6.3050 mL | 12.6100 mL | |
| 5 mM | 0.2522 mL | 1.2610 mL | 2.5220 mL | |
| 10 mM | 0.1261 mL | 0.6305 mL | 1.2610 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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