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Tobramycin/妥布霉素 {[allProObj[0].p_purity_real_show]}

货号:A976001 同义名: 托普霉素 / Nebramycin Factor 6; Deoxykanamycin B

Tobramycin是一种氨基糖苷类抗生素,具有广谱抗菌活性,由Streptomyces tenebrarius产生。

Tobramycin/妥布霉素 化学结构 CAS号:32986-56-4
Tobramycin/妥布霉素 化学结构
CAS号:32986-56-4
Tobramycin/妥布霉素 3D分子结构
CAS号:32986-56-4
Tobramycin/妥布霉素 化学结构 CAS号:32986-56-4
Tobramycin/妥布霉素 3D分子结构 CAS号:32986-56-4
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Tobramycin/妥布霉素 生物活性

描述 Tobramycin is a new aminoglycoside antibiotic with a broad antibacterial spectrum in vitro, and pharmacokinetic properties similar to those for gentamicin. Like other aminoglycoside antibiotics, tobramycin is active in vitro in low concentrations against Staphylococcus aureus. The sensitivity of P. aeruginosa to tobramycin is influenced by the magnesium, and calcium content of the culture media whilst that of all species is reduced by sodium ions[2]. Aerosolized tobramycin 100 mg/ml solution delivered higher lung dose compared to tobramycin 40 mg/ml solution[3]. When tilmicosin is used to treat clinical outbreaks of M. gallisepticum in broilers, a dosing scheme of 20 mg tilmicosin/kg BW (body weight) for five successive days seems to be the most recommended scheme[4].

Tobramycin/妥布霉素 细胞实验

Cell Line
Concentration Treated Time Description References
Pseudomonas aeruginosa CW8 8 mg/L 120 hours To evaluate the antibacterial activity of tobramycin against Pseudomonas aeruginosa CW8. Results showed that tobramycin monotherapy produced initial killing of 2-log10 CFU/ml at 7 h followed by regrowth close to the growth control by 48 h. Antimicrob Agents Chemother. 2022 Mar 15;66(3):e0220321
Pseudomonas aeruginosa CW30 2 mg/L 120 hours To evaluate the antibacterial activity of tobramycin against Pseudomonas aeruginosa CW30. Results showed that tobramycin monotherapy produced initial killing of 2-log10 CFU/ml at 7 h followed by regrowth close to the growth control by 48 h. Antimicrob Agents Chemother. 2022 Mar 15;66(3):e0220321
Neutrophils 0.001-0.5 mM 15 minutes Study the effect of tobramycin and copper-tobramycin complex on superoxide release from neutrophils. Results showed that copper-tobramycin significantly reduced detectable superoxide levels, while tobramycin had no significant effect. Br J Pharmacol. 2013 Mar;168(5):1165-81
CFBE41o2 cells 1000 μg/ml tobramycin + 1 mM deferasirox 16 hours To evaluate the effect of tobramycin in combination with iron chelators on established Pseudomonas aeruginosa biofilms. Results showed that the combination reduced biofilm biomass by 90% and viable bacteria by 7-log units. Am J Respir Cell Mol Biol. 2009 Sep;41(3):305-13
Pseudomonas aeruginosa 0.5–128 μg/ml 18–24 hours To determine the minimal inhibitory concentration (MIC) of tobramycin, results showed no interference by D-methionine on its antimicrobial efficacy. J Cyst Fibros. 2016 Jul;15(4):518-30
Staphylococcus aureus 0.5–4 μg/ml 18–24 hours To determine the minimal inhibitory concentration (MIC) of tobramycin, results showed no interference by D-methionine on its antimicrobial efficacy. J Cyst Fibros. 2016 Jul;15(4):518-30
Escherichia coli 1–64 μg/ml 18–24 hours To determine the minimal inhibitory concentration (MIC) of tobramycin, results showed no interference by D-methionine on its antimicrobial efficacy. J Cyst Fibros. 2016 Jul;15(4):518-30
Pseudomonas aeruginosa biofilm (MC75) 4 μg/ml 28 days Evaluate the antibacterial effect of tobramycin alone on mature biofilms, showing that MC75 biofilm was resistant to 4 μg/ml tobramycin. Antimicrob Agents Chemother. 2010 Oct;54(10):4409-15
Pseudomonas aeruginosa biofilm (MC99) 4 μg/ml 28 days Evaluate the antibacterial effect of tobramycin alone on mature biofilms, showing that MC99 biofilm was completely eradicated by 4 μg/ml tobramycin. Antimicrob Agents Chemother. 2010 Oct;54(10):4409-15
Pseudomonas aeruginosa biofilm (PYO2) 4 μg/ml 28 days Evaluate the antibacterial effect of tobramycin alone on mature biofilms, showing that PYO2 biofilm was resistant to 4 μg/ml tobramycin. Antimicrob Agents Chemother. 2010 Oct;54(10):4409-15
Pseudomonas aeruginosa biofilm (PYO1) 4 μg/ml 28 days Evaluate the antibacterial effect of tobramycin alone on mature biofilms, showing that PYO1 biofilm was completely eradicated by 4 μg/ml tobramycin. Antimicrob Agents Chemother. 2010 Oct;54(10):4409-15
Pseudomonas aeruginosa biofilm (PAO1) 4 μg/ml 28 days Evaluate the antibacterial effect of tobramycin alone on mature biofilms, showing that PAO1 biofilm was resistant to 4 μg/ml tobramycin. Antimicrob Agents Chemother. 2010 Oct;54(10):4409-15
Human lung microvascular endothelial cells (HLMVEC) 0.01-0.5 mM 3.5 hours Investigate the uptake mechanism and antioxidant activity of tobramycin and copper-tobramycin complex in endothelial cells. Results showed that both were taken up via heparan sulphate-dependent mechanism, and copper-tobramycin exhibited intracellular antioxidant activity. Br J Pharmacol. 2013 Mar;168(5):1165-81
CFBE41o2 cells 1000 μg/ml 30 minutes To evaluate the effect of tobramycin alone or in combination with iron chelators on established Pseudomonas aeruginosa biofilms. Results showed that tobramycin alone reduced biofilm biomass by 64%. Am J Respir Cell Mol Biol. 2009 Sep;41(3):305-13

Tobramycin/妥布霉素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Guinea pigs Tobramycin-induced ototoxicity model Subcutaneous injection 100 mg/kg/day Daily for 21 days To evaluate the protective effect of D-methionine against tobramycin-induced ototoxicity, results showed significant reductions in auditory brainstem response (ABR) threshold shifts and outer hair cell (OHC) loss. J Cyst Fibros. 2016 Jul;15(4):518-30
Saccharomyces cerevisiae Yeast cell model Culture medium addition 250 μM 48 hours Evaluate the regulatory effect of Tobramycin on GFP expression in yeast cells Nucleic Acids Res. 2023 Nov 10;51(20):11375-11385

Tobramycin/妥布霉素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02958514 Dry Eye Syndrome Not Applicable Unknown March 2017 -
NCT01319253 - Completed - United States, Indiana ... 展开 >> Indiana University Indianapolis, Indiana, United States, 46202 收起 <<
NCT02334384 Furunculosis Phase 1 Phase 2 Completed - United States, Virginia ... 展开 >> Sentara Norfolk General Hospital Norfolk, Virginia, United States, 23507 收起 <<

Tobramycin/妥布霉素 参考文献

[1]Loose M, Naber KG, et al. Urinary concentration and antimicrobial activity of tobramycin in healthy volunteers receiving a single oral dose of a novel formulation for improved absorption. Int J Antimicrob Agents. 2017 Nov 17. pii: S0924-8579(17)30396-5.

[2]Brogden RN, Pinder RM, Sawyer PR, Speight TM, Avery GS. Tobramycin: a review of its antibacterial and pharmacokinetic properties and therapeutic use. Drugs. 1976;12(3):166–200

[3]Brogden RN, Pinder RM, Sawyer PR, Speight TM, Avery GS. Tobramycin: a review of its antibacterial and pharmacokinetic properties and therapeutic use. Drugs. 1976;12(3):166–200

[4]Garmyn A, Vereecken M, De Gussem K, Depondt W, Haesebrouck F, Martel A. Efficacy of Tylosin and Tilmicosin Against Experimental Mycoplasma gallisepticum Infection in Chickens. Avian Dis. 2019;63(2):359–365

Tobramycin/妥布霉素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.69mL

2.14mL

1.07mL

21.39mL

4.28mL

2.14mL

Tobramycin/妥布霉素 技术信息

CAS号32986-56-4
分子式C18H37N5O9
分子量 467.51
SMILES Code O[C@@H]([C@@H]1O[C@@]([C@@H](C[C@@H]2O)N)([H])O[C@@H]2CN)[C@H]([C@@H](C[C@@H]1N)N)O[C@@]([C@@H]([C@@H](N)[C@@H]3O)O)([H])O[C@@H]3CO
MDL No. MFCD00077885
别名 托普霉素 ;Nebramycin Factor 6; Deoxykanamycin B; NSC 180514; Gernebcin; Distobram
运输蓝冰
InChI Key NLVFBUXFDBBNBW-PBSUHMDJSA-N
Pubchem ID 36294
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 2 mg/mL(4.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(213.9 mM)

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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