Gentamycin Sulfate
(Synonyms: 硫酸庆大霉素) 目录号 : GC15790
Gentamycin Sulfate 是一种口服活性氨基糖苷类抗生素，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。
Cas No.:1405-41-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
Mice: Bacterial challenged mice are treated with methicillin, gentamicin, both methicillin and gentamicin, or no antibiotics. The treatment is given three times a day for up to 3 days. Each dose of methicillin is 75 mg per mouse (3 g/kg of body weight), and the gentamicin dose is 0.75 mg per mouse (0.03 g/kg). The antibiotics are given subcutaneously in 0.1 or 0.5 mL of saline. Mice are sacrificed and serum and aspirate samples are collected[4]. |
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References: [1]. Xu W, 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. Anal Bioanal Chem. 2016 May;408(14):3801-9. |
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Gentamicin is an aminoglycoside antibiotic, always used the sulfate form, composed of a mixture of related gentamicin components and fractions ,which is used to treat many types of bacterial infections, particularly those caused by Gram-negative organisms.[1]
Gentamicin is a bactericidal antibiotic that works by irreversibly binding the 30S subunit of the bacterial ribosome and 16S rRNA, interrupting protein synthesis. This mechanism of action is similar to other aminoglycosides.The ribosome is a large and complex molecular machine, found within all living cells, that serves as the site of biological protein synthesis (translation). Ribosomes link amino acids together in the order specified by messenger RNA (mRNA) molecules. [2] Ribosomes consist of two major components, the small ribosomal subunit which reads the RNA, and the large subunit which joins amino acids to form a polypeptide chain. Each subunit is composed of one or more ribosomal RNA (rRNA) molecules and a variety of proteins. Ribosomes differ in their size, sequence, structure, and the ratio of protein to RNA from bacteria, archaea and eukaryotes (the three domains of life on Earth).[3] The differences in structure allow some antibiotics to kill bacteria by inhibiting their ribosomes, while leaving human ribosomes unaffected. Gentamicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12 which interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. The interaction with the wobble base in the anticodon of tRNA leads to interference with the initiation complex misreading, so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.[4]
Gentamicin is a broad spectrum aminoglycoside antibiotic. Aminoglycosides are useful primarily in infection diease include aerobic, Gram-negative bacteria, In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. Symptoms of gentamicin toxicity include: Balance difficulty, Bouncing, unsteady vision, Ringing in the ears (tinnitus), Difficulty multi-tasking, particularly when standing.[5] Gentamicin is very poorly absorbed orally. Injections lead to peak serum concentrations in 30-60 minutes.
References:
1. Moulds, Robert and Jeyasingham, Melanie "Gentamicin: a great way to start". Australian Prescriber 2010 (33): 134–135.
2. Czernilofsky. et al. "PROTEINS AT TRANSFER-RNA BINDING-SITES OF ESCHERICHIA-COLI RIBOSOMES". NATL ACAD SCIENCES. 1974, 71 (1): 230–234.
3. Ben-Shem A. et al. "The structure of the eukaryotic ribosome at 3.0 Å resolution". 2011 Science 334 (6062): 1524–1529.
4. Lopez-Novoa, Jose. "New insights into the mechanism of aminoglycoside nephrotoxicity: an integrative point of view." 2011. Kidney International.
5. Pandya, A. et al. (1993)."Nonsyndromic Hearing Loss and Deafness, Mitochondrial". Book.
| 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。
Oral Gentamycin Sulfate in treatment of infantile diarrhea due to enteropathogenic E. coli
Clin Pediatr (Phila) 1970 Sep;9(9):510-1.4916527 10.1177/000992287000900906
[Pharmacokinetics of Gentamycin Sulfate in the healthy and in patients with terminal renal failure]
Dtsch Med Wochenschr 1971 Apr 23;96(17):734-8 passim.4994837 10.1055/s-0028-1108321
Development of a novel bead-based 96-well filtration plate competitive immunoassay for the detection of Gentamycin
Biosens Bioelectron 2013 Nov 15;49:126-32.23728198 10.1016/j.bios.2013.04.027
We developed a sensitive, simple, inexpensive and rapid bead-based immunoassay platform, composed of liposomal nanovesicle amplification system, Gentamycin Sulfate beads and 96-well filtration plates. In the beginning of the assay, Gentamycin Sulfate beads, Gentamycin Sulfate and Gentamycin specific antibody were incubated in a bottom-sealed 96-well filtration plate. After incubation, washing was done by running washing buffer through the unsealed filtration plate with only gravity and the antibody-Gentamycin bead complexes were retained in the plate. Fluorescent dye-loaded protein G-liposomal nanovesicles were then added to specifically bind to antibodies on the retained beads. After washing unbound nanovesicles, millions of fluorescent dye molecules were released by adding a detergent solution to lyse liposomal nanovesicles. The limit of detection (LOD) of this novel detection platform in TBS and in skim milk were 52.65 ng/mL and 14.16 ng/mL, which are both sufficient for detecting the 200 ng/mL Codex maximum residual level (MRL). The dynamic ranges were both from each of their LODs to 100 渭g/mL. The 50% inhibition concentrations (IC50) in TBS and skim milk were 199.66 ng/mL and 360.81 ng/mL, respectively. We also demonstrated the good specificity of this platform by comparing detection results between pure Gentamycin solution and a mixture solution of 6 different antibiotics including Gentamycin in skim milk. The entire assay with 60 samples was conducted within 2h. In sum, this novel biosensing platform not only fulfilled most benefits of magnetic bead-based assays, but also was inexpensive and convenient by replacing the magnetic separation with filtration plate separation.
[Prolonged-action Gentamycin Sulfate eyedrops]
Antibiotiki 1981 Jan;26(1):60-4.7212685
A new dosage form of gentamicin, 0.3 per cent eye drops with polyglucin was developed. Its pharmacokinetics and chemotherapeutic properties were studied. It was shown that in the form of eye drops gentamicin has a prolonged action, provides high levels of penetration into the eye tissues and is effective in the treatment of eye infections.
In vitro release kinetics of gentamycin from a sodium hyaluronate gel delivery system suitable for the treatment of peripheral vestibular disease
Drug Dev Ind Pharm 1999 Jan;25(1):15-20.10028414 10.1081/ddc-100102137
For certain patients who experience intense vertigo arising from unilateral vestibular lesions, the primary therapy is a vestibular nerve section, an intracranial surgical procedure. One alternative to this treatment is therapeutic ablation of vestibular function on the unaffected side using an ototoxic agent. We prepared a biodegradable sustained-release gel delivery system using sodium hyaluronate that can be administered into the middle ear using only a local anesthetic. The gel contains Gentamycin Sulfate, the ototoxic agent of choice for treatment of unilateral vestibulopathy, and it exhibits diffusion-controlled release of the drug over a period of hours. The released gentamycin could then diffuse into the inner ear through the round membrane. This represents an important advance over previous formulations, which used only Gentamycin Sulfate solutions, in that it should allow more careful control of the dose, it should reduce loss of the drug from the middle ear site, and it should maintain intimate contact with the round membrane. By carefully controlling the dose, it should be possible to inhibit vestibular function while minimizing hearing loss. Herein we describe the in vitro release kinetics of Gentamycin Sulfate from sodium hyaluronate gels and find that the system obeys Fickian behavior.