Tobramycin | 妥布霉素

MCE 国际站：Tobramycin

中文名：妥布霉素

CAS：32986-56-4

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：Tobramycin（Nebramycin Factor 6）是一种肠胃外给药的广谱氨基糖苷类抗生素，广泛用于治疗由敏感微生物引起的中度至重度细菌感染^[1]。

体外：Tobramycin (0-50 ng/mL；24 小时) 与脓肿分枝杆菌酶 (PodA) 联合使用可显著降低铜绿假单胞菌细胞活力[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Tobramycin (50-400 mg/kg/天，腹腔注射，每4小时一次) 在小鼠肺炎模型中，与 Meropenem (HY-13678) 联合使用能够在低剂量下产生细菌细胞杀伤作用[3]。 Tobramycin (皮下注射注射，单次给药) 在小鼠和大鼠中半数致死剂量分别为 441 和 969 mg/kg[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Murine Model of Pseudomonas aeruginosa Pneumonia Female, Swiss-Webster mice [3] Dosage: 50, 100, 150, 214, and 400 mg/kg/day Administration: Intraperitoneal injection (i.p.) ,once every 4h Result: Had near-maximal killing of the wild-type bacteria occurred at approximately 150 mg/kg/day when tobramycin alone. Combinated with Meropenem (HY-13678) produced near-maximal effect (i.e., bacterial cell kill) at low doses of both drugs (60 and 50 mg/kg/day for Meropenem (HY-13678) and tobramycin, respectively). Animal Model: Mice, rats, cats and dogs for toxicologic evaluation[4] Dosage: 7.5,15,30,120,441,969 mg/kg Administration: Subcutaneous injection (s.c.), Intravenous injection (i.v.) ,Intramuscular injection(i.m.) Result: The s.c. LD50 values in mice and rats were 441 and 969 mg/kg, respectively. Within 1 hour after treated, death with central nervous system depression as a precursor occurred in rats and mice. A 100 mg/kg iv dose in chloraloseanesthetized catsproduced a moderate, transient decreasein blood pressure and a significant decrease in inspiratory volume and soleus twitch force. Changed renal tissue in rats which were given daily sc doses of 15-120 mg/kg for 3 months. im dose of 7.5 mg/kg for a l-month had no apparent effect on dogs, but a 30 mg/kg dose for a l-month produced severerenal damage. Clinical Trial

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研究领域：Anti-infection

作用靶点：Bacterial  |  Antibiotic

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参考文献：[1]. Tobramycin.

[2]. VanDrisse CM, et.al. Computationally designed pyocyanin demethylase acts synergistically with tobramycin to kill recalcitrant Pseudomonas aeruginosa biofilms. Proc Natl Acad Sci U S A. 2021 Mar 23;118(12):e2022012118.

[3]. Louie A, et.al. Impact of meropenem in combination with tobramycin in a murine model of Pseudomonas aeruginosa pneumonia. Antimicrob Agents Chemother. 2013 Jun;57(6):2788-92. 

[4]. Welles JS, et.al. Preclinical toxicology studies with tobramycin. Toxicol Appl Pharmacol. 1973 Jul;25(3):398-409.