| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Aminoglycoside
Tobramycin sulfate targets the bacterial 30S ribosomal subunit, specifically binding to a site on the 16S rRNA. It binds irreversibly to this aminoglycoside receptor and fixes the 30S-50S ribosomal complex at the start codon, interfering with the initiation of protein synthesis. This action prevents the formation of the functional 70S initiation complex. In addition to inhibiting initiation, tobramycin causes misreading of the mRNA template, resulting in the incorporation of incorrect amino acids and the production of abnormal, nonfunctional proteins. The drug may also inhibit the activity of certain enzymes, such as DNA polymerase and topoisomerase. |
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| ln Vitro |
In vitro, tobramycin sulfate exhibits bactericidal activity against a number of gram-negative bacteria. Its mechanism involves binding to the 30S ribosomal subunit and blocking the formation of peptide bonds. It is especially effective against species of *Pseudomonas*. In laboratory experiments, it has been used as a reagent in biochemical and physiological studies. The minimum inhibitory concentration (MIC) varies depending on the bacterial strain. Tobramycin's activity is concentration-dependent, and it exhibits a post-antibiotic effect.
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| ln Vivo |
In vivo, tobramycin is used as a potent antibiotic for treating various types of bacterial infections, particularly gram-negative infections. The provided search results do not detail specific in vivo activity data for tobramycin sulfate itself. However, it is known for its clinical efficacy against severe gram-negative infections. In research, systemic exposure to tobramycin after local antibiotic treatment has been investigated. Its pharmacokinetic parameters, such as half-life (approximately 1.8 hours) and volume of distribution (0.297 L/kg), have been characterized.
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| Enzyme Assay |
Non-cellular enzyme/receptor binding assays for tobramycin sulfate are typically not performed, as it is an antibiotic whose primary mechanism of action is on the bacterial ribosome. However, its activity can be assessed by measuring its binding affinity to the 30S ribosomal subunit using techniques like surface plasmon resonance (SPR) or by evaluating its ability to inhibit protein synthesis in cell-free systems using radiolabeled amino acids.
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| Cell Assay |
In vitro cellular assays for tobramycin sulfate are performed by culturing susceptible bacteria and measuring the minimum inhibitory concentration (MIC). The antibiotic's bactericidal activity is assessed by determining the reduction in bacterial colony-forming units (CFUs) after treatment. Time-kill curve studies can also be conducted to evaluate the rate and extent of bacterial killing. It may also be used in cell culture to study its effects on eukaryotic cells, though this is not its primary application.
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| Animal Protocol |
In vivo animal experiments for tobramycin sulfate have been conducted in laboratory animals to evaluate its toxicity and efficacy. For instance, the nephrotoxic and ototoxic effects of tobramycin have been studied in young adult and aged female rats and in multiple-dose studies. These studies help to establish safety and pharmacokinetic profiles. Efficacy studies are typically performed in animal models of infection, such as the murine thigh infection model or pneumonia models.
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| ADME/Pharmacokinetics |
Tobramycin sulfate has a molecular weight of 565.59 and a molecular formula of C18H37N5O9•H2SO4. Following active transport into the cell, it binds to the 30S ribosomal subunit. The CAS number is 49842-07-1, and the UNII code is HJT0RXD7JK. It is available for research use only and is not intended for diagnostic or therapeutic use. The compound is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
The toxicological profile of tobramycin sulfate includes potential nephrotoxic and ototoxic effects, which have been studied in animal models. Its safety has been evaluated in single and multiple administrations to laboratory animals. As an aminoglycoside antibiotic, it is known to have these dose-limiting toxicities, which are a key consideration in its clinical use. The risk of toxicity is related to the cumulative dose and duration of therapy.
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| References | |
| Additional Infomation |
Tobramycin sulfate may cause developmental toxicity depending on state or federal labeling requirements. Tobramycin sulfate is the sulfate salt of tobramycin, an aminoglycoside antibiotic derived from Streptomyces tenebrarius, possessing bactericidal activity. After entering the cell via active transport, tobramycin irreversibly binds to specific aminoglycoside receptors on the bacterial 30S ribosomal subunit, fixing the 30S-50S ribosomal complex at the start codon (AUG), thereby interfering with the initiation of protein synthesis. Furthermore, the drug can induce misreading of the mRNA template, leading to: 1) ribosomal complex dissociation and inhibition of protein elongation; or 2) incorporation of incorrect amino acids into the elongating polypeptide chain, resulting in abnormal or nonfunctional proteins. Cell permeability is altered, ultimately leading to cell death. Tobramycin sulfate is a broad-spectrum aminoglycoside antibiotic produced by Streptomyces tenebrarius. It is effective against Gram-negative bacteria, particularly Pseudomonas. It is a 10% component of nebramycin, an antibiotic complex produced by the same bacteria.
See also: tobramycin sulfate (note moved here). Tobramycin sulfate (NSC-180514) is an aminoglycoside antibiotic agent and protein synthesis inhibitor. It binds to the 30S and 50S ribosome and prevents formation of the 70S complex. It is an aminoglycoside antibiotic with efficacy against gram-negative bacteria. No specific information on clinical trials beyond its established use as an antibiotic is detailed in the provided search results. It is a well-established drug with a long history of clinical use. |
| Molecular Formula |
C18H37N5O9.5/2H2O4S
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|---|---|
| Molecular Weight |
712.18
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| Exact Mass |
565.226
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| Elemental Analysis |
C, 38.23; H, 6.95; N, 12.38; O, 36.77; S, 5.67
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| CAS # |
49842-07-1
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| Related CAS # |
Tobramycin;32986-56-4; 79645-27-5 (sulfate deleted); 49842-07-1 (sulfate)
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| PubChem CID |
62005
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| Appearance |
White to off-white solid powder
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| Density |
1.52g/cm3
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| Boiling Point |
775.4ºC at 760mmHg
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| Flash Point |
422.8ºC
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
691
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| Defined Atom Stereocenter Count |
14
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| SMILES |
C1[C@@H]([C@H]([C@@H]([C@H]([C@@H]1N)O[C@@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)N)O)O)O[C@@H]3[C@@H](C[C@@H]([C@H](O3)CN)O)N)N.OS(=O)(=O)O
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| InChi Key |
ZEUUPKVZFKBXPW-TWDWGCDDSA-N
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| InChi Code |
InChI=1S/C18H37N5O9.H2O4S/c19-3-9-8(25)2-7(22)17(29-9)31-15-5(20)1-6(21)16(14(15)28)32-18-13(27)11(23)12(26)10(4-24)30-18;1-5(2,3)4/h5-18,24-28H,1-4,19-23H2;(H2,1,2,3,4)/t5-,6+,7+,8-,9+,10+,11-,12+,13+,14-,15+,16-,17+,18+;/m0./s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-4-amino-2-[(1S,2S,3R,4S,6R)-4,6-diamino-3-[(2R,3R,5S,6R)-3-amino-6-(aminomethyl)-5-hydroxyoxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-6-(hydroxymethyl)oxane-3,5-diol;sulfuric acid
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| Synonyms |
TOBRAMYCIN SULFATE; Gernebcin; Nebcin; 49842-07-1; Nebicina;
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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 |
| 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 (351.03 mM)
DMSO: < 1 mg/mL |
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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 | 1.4041 mL | 7.0207 mL | 14.0414 mL | |
| 5 mM | 0.2808 mL | 1.4041 mL | 2.8083 mL | |
| 10 mM | 0.1404 mL | 0.7021 mL | 1.4041 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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