Gentamycin Sulfate
(Synonyms: 硫酸庆大霉素) 目录号 : GC15790
硫酸庆大霉素（Gentamycin Sulfate）是一种氨基糖苷类抗生素，可抑制革兰氏阳性和革兰氏阴性细菌的生长，并抑制组织培养中的几种支原体菌株。Gentamicin sulfate可抑制脱氧核糖核酸酶（DNase I）的活性，IC50值为0.57±0.12mM。
Cas No.:1405-41-0
Sample solution is provided at 25 µL, 10mM.
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Gentamycin sulfate is an aminoglycoside antibiotic that inhibits the growth of Gram-positive and Gram-negative bacteria and several strains of mycoplasma in tissue culture[1]. Gentamicin sulfate inhibits the activity of deoxyribonuclease I with an IC50 value of 0.57±0.12mM[2]. Gentamycin sulfate acts as a protein synthesis inhibitor, binding irreversibly to the small 16S rRNA of the 30S ribosomal subunit and interfering with protein synthesis, a mechanism of action similar to that of other aminoglycosides[3]. Gentamycin sulfate is used to treat a variety of bacterial infections. It is poorly absorbed orally and can be administered intramuscularly or intravenously[4]. Gentamycin sulfate is a potent antibiotic that is widely used in human and animal cell culture. The recommended concentration is usually 50μg/ml, but caution is required when using it in plant cell lines. The recommended concentration is 10μg/ml or lower [5, 6].
In vitro, treatment of human neutrophils with gentamycin sulfate (0-200μM) for 1h significantly inhibited NADPH oxidase activity and concentration-dependently inhibited superoxide production in neutrophils exposed to phorbol myristate [5]. Gentamycin Sulfate (25, 100, 400 μg/mL) treated human osteoblasts (hFOB 1.19) for 6 hours, dose-dependently reduced alkaline phosphatase (ALP) activity, inhibited cell proliferation, survival and adhesion ability [6].
In vivo, gentamycin sulfate (50, 100 mg/kg/day) was intravenously injected into male Sprague Dawley rats for 7 days, which led to increased expression of kidney injury molecule 1 (KIM-1) and neutrophil gelatinase-associated lipocalin (NGAL) in a dose- and time-dependent manner, inducing a rat nephrotoxicity model [7].
References:
[1] Rudin A, Healey A, Phillips C A, et al. Antibacterial activity of gentamicin sulfate in tissue culture[J]. Applied microbiology, 1970, 20(6): 989-990.
[2] Xu W, Xie Z, Tong C, et al. A rapid and sensitive method for kinetic study and activity assay of DNase I in vitro based on a GO-quenched hairpin probe[J]. Analytical and Bioanalytical Chemistry, 2016, 408: 3801-3809.
[3] Kumar C, Himabindu M, Jetty A. Microbial biosynthesis and applications of gentamicin: a critical appraisal[J]. Critical reviews in biotechnology, 2008, 28(3): 173-212.
[4] Nwakile D C, Dozie-Nwakile O C, Okoye E I, et al. Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation[J]. European Pharmaceutical Journal, 2021, 68(2): 8-15.
[5] Schafer T W, Pascale A, Shimonaski G, et al. Evaluation of gentamicin for use in virology and tissue culture[J]. Applied Microbiology, 1972, 23(3): 565-570.
[6] Dodds J H, Roberts L W. Some inhibitory effects of gentamicin on plant tissue cultures[J]. In Vitro, 1981, 17: 467-470.
[7] Umeki S. Anti-inflammatory action of gentamycin through inhibitory effect on neutrophil NADPH oxidase activity[J]. Comparative Biochemistry and Physiology Part B: Biochemistry and Molecular Biology, 1995, 110(4): 817-821.
[8] Ince A, Schütze N, Hendrich C, et al. In vitro investigation of orthopedic titanium-coated and brushite-coated surfaces using human osteoblasts in the presence of gentamycin[J]. The Journal of arthroplasty, 2008, 23(5): 762-771.
[9] Luo Q H, Chen M L, Chen Z L, et al. Evaluation of KIM-1 and NGAL as early indicators for assessment of gentamycin-induced nephrotoxicity in vivo and in vitro[J]. Kidney and Blood Pressure Research, 2016, 41(6): 911-918.
硫酸庆大霉素（Gentamycin Sulfate）是一种氨基糖苷类抗生素，可抑制革兰氏阳性和革兰氏阴性细菌的生长，并抑制组织培养中的几种支原体菌株[1]。Gentamicin sulfate可抑制脱氧核糖核酸酶（DNase I）的活性，IC50值为0.57±0.12mM[2]。Gentamycin Sulfate起到蛋白质合成抑制剂的作用，不可逆地与30S核糖体亚基的小16S rRNA结合，干扰蛋白质合成，这种作用机制类似于其他氨基糖苷类药物[3]。Gentamycin Sulfate用于治疗多种类型的细菌感染，口服吸收差，可以通过肌肉或静脉注射给药[4]。Gentamycin Sulfate是一种有效的抗生素，广泛应用于人类和动物细胞培养中，通常推荐的浓度为50μg/ml，但在植物细胞系中使用时需要谨慎，推荐浓度为10μg/ml或更低[5, 6]。
在体外，Gentamycin Sulfate（0-200μM）处理人类中性粒细胞1h，显著抑制了NADPH氧化酶活性，浓度依赖性地抑制了暴露于佛波醇肉豆蔻酸酯的中性粒细胞的超氧化物生成[7]。Gentamycin Sulfate（25、100、400μg/mL）处理人成骨细胞（hFOB 1.19）6h，剂量依赖性地降低了碱性磷酸酶（ALP）活性，抑制了细胞的增殖、存活和粘附能力[8]。
在体内，Gentamycin Sulfate（50，100mg/kg/day）通过静脉注射处理雄性Sprague Dawley大鼠7天，剂量和时间依赖性地导致了肾损伤分子1（KIM-1）和中性粒细胞明胶酶相关脂质运载蛋白（NGAL）表达增加，诱导了大鼠肾毒性模型[9]。
| Cell experiment [1]: | |
Cell lines | Human neutrophils |
Preparation Method | Cells were incubated with gentamycin sulfate (0-200μM) for 1 hour. |
Reaction Conditions | 0-200μM; 1h |
Applications | Gentamycin Sulfate inhibits superoxide production in neutrophils exposed to phorbol myristate in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (180-220g) were housed under conditions of 23±2°C and 40-70% relative humidity at all times in an alternating 12h light-dark cycle. Gentamicin sulfate was intravenously administered at 0, 50 or 100 mg/kg/day and the animals were necropsied on days 1, 3 or 7 for toxicity evaluation. |
Dosage form | 0, 50 or 100 mg/kg/day; i.v. |
Applications | Repeated administration of Gentamicin to rats for 1, 3, or 7 days resulted in a dose- and time-dependent increase in the expression of KIM-1 and NGAL. |
References: | |
| Cas No. | 1405-41-0 | SDF | |
| 别名 | 硫酸庆大霉素 | ||
| 化学名 | sulfuric acid compound with (2R,3R,4R,5R)-2-(((1S,2S,3R,4S,6R)-4,6-diamino-3-(((2R,3R,6R)-3-amino-6-((R)-1-(methylamino)ethyl)tetrahydro-2H-pyran-2-yl)oxy)-2-hydroxycyclohexyl)oxy)-5-methyl-4-(methylamino)tetrahydro-2H-pyran-3,5-diol and (2R,3R,4R,5R)-2-( | ||
| Canonical SMILES | C[C@]1(O)CO[C@H](O[C@H]2[C@H](N)C[C@H](N)[C@@H](O[C@H]3O[C@@]([H])([C@@H](C)NC)CC[C@H]3N)[C@@H]2O)[C@H](O)[C@H]1NC.C[C@]4(O)CO[C@H](O[C@H]5[C@H](N)C[C@H](N)[C@@H](O[C@H]6O[C@H](CN)CC[C@H]6N)[C@@H]5O)[C@H](O)[C@H]4NC.C[C@]7(O)CO[C@H](O[C@H]8[C@H](N)C[C@H]( | ||
| 分子式 | C21H43N5O7·H2SO4 | 分子量 | 575.67 |
| 溶解度 | ≥ 51.1mg/mL in Water | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7371 mL | 8.6855 mL | 17.3711 mL |
| 5 mM | 0.3474 mL | 1.7371 mL | 3.4742 mL |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7371 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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