| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Micronomicin targets the bacterial ribosome, specifically binding to the 30S ribosomal subunit. By binding to this subunit, it interferes with bacterial protein synthesis, causing misreading of mRNA and ultimately inhibiting bacterial cell growth and propagation. This mechanism is characteristic of the aminoglycoside class of antibiotics, which disrupt the fidelity of translation and lead to the production of non-functional or toxic proteins. The drug's bactericidal activity is concentration-dependent and exhibits a post-antibiotic effect.
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| ln Vitro |
Gram-positive and Gram-negative bacteria are both susceptible to the broad antibacterial spectrum of micronomicin [1].
In vitro, Micronomicin demonstrates potent antibacterial and bactericidal activity against a broad spectrum of bacterial pathogens. It is effective against various Gram-negative organisms, including Escherichia coli, Klebsiella, and Pseudomonas species, as well as Gram-positive organisms such as Staphylococcus aureus. Its minimum inhibitory concentrations (MICs) against susceptible strains are typically in the range of 0.5-4 µg/mL. The compound shows synergistic effects when combined with other antibiotics and exhibits activity against some aminoglycoside-resistant strains. |
| ln Vivo |
In vivo, Micronomicin is clinically used for the treatment of systemic bacterial infections. It has been shown to be effective in animal models of sepsis and localized infections. Clinical studies have demonstrated its efficacy in treating respiratory tract infections, urinary tract infections, and biliary tract infections, as well as more severe conditions such as sepsis, empyema, and pelvic inflammatory disease. The drug's clinical utility is supported by its broad spectrum and potent bactericidal activity.
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| Enzyme Assay |
The in vitro antibacterial activity of Micronomicin is assessed using standard broth microdilution or agar dilution methods following CLSI guidelines. Serial two-fold dilutions of the compound are prepared in 96-well plates with cation-adjusted Mueller-Hinton broth. A standardized bacterial inoculum (approximately 5×10⁵ CFU/mL) is added to each well, and the plates are incubated at 35°C for 16-20 hours. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible bacterial growth. For cell-free protein synthesis inhibition assays, bacterial ribosomes are incubated with radiolabeled amino acids in the presence of the compound, and the incorporation into nascent polypeptides is measured.
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| Cell Assay |
For cellular assays, bacterial cultures of target pathogens are grown to logarithmic phase in appropriate media. Cells are treated with various concentrations of Micronomicin (typically ranging from 0.125 to 64 µg/mL) for defined periods (e.g., 2-24 hours). Bacterial viability is assessed by colony counting on agar plates or by using metabolic assays such as the MTT reduction assay. The effect on protein synthesis can be evaluated by measuring the incorporation of ³H-leucine or ³H-methionine into newly synthesized proteins. Time-kill curves are generated by sampling at multiple time points to determine the bactericidal kinetics.
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| Animal Protocol |
In vivo efficacy studies are conducted in murine models of systemic infection. Mice are injected intraperitoneally with a lethal dose of a bacterial pathogen (e.g., E. coli or P. aeruginosa). Micronomicin is administered via subcutaneous or intramuscular injection at various doses (typically 1-50 mg/kg) either as a single dose or in divided doses over 24-48 hours. The primary endpoint is the survival rate over 7 days. Additional endpoints include the reduction of bacterial burden in target organs (spleen, liver, lungs) as determined by quantitative culture. Pharmacodynamic parameters such as the ratio of peak concentration to MIC (Cmax/MIC) and area under the curve to MIC (AUC/MIC) are correlated with efficacy.
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| ADME/Pharmacokinetics |
Micronomicin is administered via intramuscular or intravenous injection, as it is poorly absorbed after oral administration. It is distributed widely in body fluids and tissues, achieving therapeutic concentrations in the lungs, kidneys, and bile. The drug is primarily excreted unchanged in the urine via glomerular filtration, with a half-life of approximately 2-3 hours in patients with normal renal function. Its elimination is prolonged in patients with renal impairment, requiring dose adjustment. The volume of distribution is approximately 0.3 L/kg.
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| Toxicity/Toxicokinetics |
The primary toxicity of Micronomicin is nephrotoxicity (renal damage) and ototoxicity (vestibular and auditory damage), which are characteristic of aminoglycoside antibiotics. The risk of toxicity is dose-dependent and related to cumulative exposure, peak serum concentrations, and duration of therapy. Nephrotoxicity typically manifests as elevated serum creatinine and reduced glomerular filtration rate. Ototoxicity may result in hearing loss or balance disturbances. The drug should be used with caution in patients with pre-existing renal impairment and in combination with other nephrotoxic agents. Neuromuscular blockade is a potential adverse effect, particularly at high doses.
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| References |
[1]. Ohkoshi M, et al. Review [new antibiotics series III]: micronomicin (author's transl). Jpn J Antibiot. 1982 Mar;35(3):691-703.
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| Additional Infomation |
Gentamicin C2b is an aminoglycoside antibiotic. Sagamicin is an aminoglycoside antibiotic marketed in Japan under the trade names Sagamicin and Luxomicina. Sagamicin is an aminoglycoside antibiotic isolated from non-reducing Micromonospora sagamiensis var. nonreducans. It is an analogue of gentamicin and exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria.
Micronomicin is a clinically approved aminoglycoside antibiotic used primarily in Asia for the treatment of various bacterial infections. It is available in injectable formulations for systemic use and is sometimes administered topically for superficial infections. The drug is generally reserved for serious infections due to its toxicity profile and is often used when other antibiotics are ineffective or contraindicated. It is not approved for use in the United States or Europe but remains an important therapeutic option in some regions for the treatment of multidrug-resistant infections. |
| Molecular Formula |
C20H41N5O7
|
|---|---|
| Molecular Weight |
463.576
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| Exact Mass |
463.301
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| CAS # |
52093-21-7
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| Related CAS # |
Micronomicin sulfate;66803-19-8
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| PubChem CID |
3037206
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.32g/cm3
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| Boiling Point |
667.2ºC at 760 mmHg
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| Flash Point |
357.3ºC
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| Index of Refraction |
1.589
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| LogP |
-4.5
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
607
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| Defined Atom Stereocenter Count |
12
|
| SMILES |
C[C@@]1(CO[C@@H]([C@@H]([C@H]1NC)O)O[C@H]2[C@@H](C[C@@H]([C@H]([C@@H]2O)O[C@@H]3[C@@H](CC[C@@H](CNC)O3)N)N)N)O
|
| InChi Key |
DNYGXMICFMACRA-XHEDQWPISA-N
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| InChi Code |
InChI=1S/C20H41N5O7/c1-20(28)8-29-19(14(27)17(20)25-3)32-16-12(23)6-11(22)15(13(16)26)31-18-10(21)5-4-9(30-18)7-24-2/h9-19,24-28H,4-8,21-23H2,1-3H3/t9-,10+,11-,12+,13-,14+,15+,16-,17+,18+,19+,20-/m0/s1
|
| Chemical Name |
(2R,3R,4R,5R)-2-[(1S,2S,3R,4S,6R)-4,6-diamino-3-[(2R,3R,6S)-3-amino-6-(methylaminomethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol
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| Synonyms |
KW 1062; KW-1062; Micronomicin
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
H2O : ~250 mg/mL (~539.29 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (107.86 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1571 mL | 10.7856 mL | 21.5712 mL | |
| 5 mM | 0.4314 mL | 2.1571 mL | 4.3142 mL | |
| 10 mM | 0.2157 mL | 1.0786 mL | 2.1571 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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