| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Carbomycin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, acting as a peptidyl transferase inhibitor.
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|---|---|
| ln Vitro |
Carbomycin exhibits inhibitory activity against various Gram-positive bacteria and Mycoplasma. It shows cross-resistance with erythromycin. It inhibits the peptidyl transferase reaction in cell-free translation systems, achieving approximately 95% inhibition of peptidyl transferase activity at a concentration of 200 μM.
|
| ln Vivo |
Carbomycin is primarily used in veterinary medicine for treating bacterial infections. Data on its human clinical application and in vivo efficacy are limited.
|
| Enzyme Assay |
1. Prepare a cell-free translation system using E. coli extracts, purified ribosomal subunits, or reconstituted components. 2. Incorporate a radiolabeled amino acid (e.g., [³H]-leucine or [¹⁴C]-phenylalanine) into the translation reaction. 3. Incubate with varying concentrations of carbomycin (0-200 μM) at 37°C for a defined time. 4. Measure nascent peptide synthesis by liquid scintillation or autoradiography after gel electrophoresis. 5. Calculate the percent inhibition of peptidyl transferase activity.
|
| Cell Assay |
1. Culture bacterial strains such as S. aureus and S. pneumoniae in Mueller-Hinton broth to logarithmic growth phase. 2. Prepare serial two-fold dilutions of carbomycin using the microbroth dilution method. 3. Inoculate with bacterial suspension and incubate at 35-37°C for 18-24 hours. 4. Determine the Minimum Inhibitory Concentration (MIC). 5. Perform colony counting on agar plates to generate time-kill curves.
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| Animal Protocol |
1. Use ICR or BALB/c mice to establish a systemic infection model by intraperitoneal injection of S. aureus. 2. Administer carbomycin via subcutaneous or intraperitoneal injection. 3. Monitor survival daily for 7-10 days. 4. After euthanasia, collect spleen, liver, and kidney tissues, homogenize, and perform colony counts on agar plates to assess bacterial clearance.
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| ADME/Pharmacokinetics |
As a veterinary macrolide antibiotic, it is expected to exhibit variable absorption, extensive tissue distribution, and hepatic metabolism. Specific human pharmacokinetic parameters are limited in the public literature.
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| Toxicity/Toxicokinetics |
5287879 mouse LD50 subcutaneous 2950 mg/kg Antibiotics and Chemotherapy, 3(117), 1953
5287879 mouse LD50 intramuscular 1 gm/kg Antibiotics and Chemotherapy, 3(117), 1953 5287879 mouse LD50 oral 3500 mg/kg Antibiotics Annual., 2(336), 1954/1955 5287879 mouse LD50 intravenous 550 mg/kg Antibiotics and Chemotherapy, 3(117), 1953 As a macrolide antibiotic, potential risks include hypersensitivity reactions, hepatotoxicity, and effects on intestinal microbiota. Human toxicity data are limited, primarily based on veterinary application experience. |
| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/5287879
|
| Additional Infomation |
Carbomycin, also known as magnamycin, is a crystalline macrolide antibiotic. This antibacterial drug is extracted from Streptomyces halstedii and exhibits strong inhibitory activity against Gram-positive bacteria and certain mycoplasma strains. The structure of Carbomycin was determined by Robert Woodward in 1957 and modified in 1965.
Molecular Weight: 841.989 g/mol; Molecular Formula: C42H67NO16; CAS Number: 4564-87-8; Density: 1.24 g/cm³. For research use only, not for human therapeutic use. |
| Molecular Formula |
C42H67NO16
|
|---|---|
| Molecular Weight |
841.97848
|
| Exact Mass |
841.446
|
| Elemental Analysis |
C, 59.91; H, 8.02; N, 1.66; O, 30.40
|
| CAS # |
4564-87-8
|
| PubChem CID |
5287879
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.24g/cm3
|
| Boiling Point |
892.2ºC at 760mmHg
|
| Melting Point |
214ºC
|
| Flash Point |
493.4ºC
|
| Index of Refraction |
1.535
|
| LogP |
2.432
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
59
|
| Complexity |
1470
|
| Defined Atom Stereocenter Count |
17
|
| SMILES |
CC(C)CC(=O)OC1C(C)OC(CC1(C)O)OC2C(C)OC(C(C2N(C)C)O)O[C@H]3[C@@H](CC=O)C[C@@H](C)C(=O)C=C[C@H]4[C@H](C[C@@H](C)OC(=O)C[C@H]([C@@H]3OC)OC(=O)C)O4
|
| InChi Key |
FQVHOULQCKDUCY-OGHXVOSASA-N
|
| InChi Code |
InChI=1S/C42H67NO16/c1-21(2)16-32(47)57-40-25(6)53-34(20-42(40,8)50)58-37-24(5)54-41(36(49)35(37)43(9)10)59-38-27(14-15-44)17-22(3)28(46)12-13-29-30(56-29)18-23(4)52-33(48)19-31(39(38)51-11)55-26(7)45/h12-13,15,21-25,27,29-31,34-41,49-50H,14,16-20H2,1-11H3/b13-12+/t22-,23-,24-,25+,27+,29+,30+,31-,34+,35-,36-,37-,38+,39+,40+,41+,42-/m1/s1
|
| Chemical Name |
[(2S,3S,4R,6S)-6-[(2R,3S,4R,5R,6S)-6-[[(1S,3R,7R,8S,9S,10R,12R,14E,16S)-7-acetyloxy-8-methoxy-3,12-dimethyl-5,13-dioxo-10-(2-oxoethyl)-4,17-dioxabicyclo[14.1.0]heptadec-14-en-9-yl]oxy]-4-(dimethylamino)-5-hydroxy-2-methyloxan-3-yl]oxy-4-hydroxy-2,4-dimethyloxan-3-yl] 3-methylbutanoate
|
| Synonyms |
CARBOMYCIN; Magnamycin; Magnamycin A; Carbomicina; ...; 4564-87-8;
|
| 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)
|
| 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
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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 | 1.1877 mL | 5.9384 mL | 11.8768 mL | |
| 5 mM | 0.2375 mL | 1.1877 mL | 2.3754 mL | |
| 10 mM | 0.1188 mL | 0.5938 mL | 1.1877 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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