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Sisomicin sulfate Sale

(Synonyms: 硫酸西索米星) 目录号 : GC32263

Sisomicin sulfate是一种由伊诺单孢菌(Micromonospora inyoensis)产生的天然氨基糖苷类抗生素,对革兰氏阳性菌具有很强的活性。

Sisomicin sulfate Chemical Structure

Cas No.:53179-09-2

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10mM (in 1mL Water)
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Sample solution is provided at 25 µL, 10mM.

Description

Sisomicin sulfate is a naturally occurring aminoglycoside antibiotic produced by Micromonospora inyoensis and has strong activity against Gram-positive bacteria[1].

In vitro, Compared to the wild-type Mycobacterium smegmatis, the PdtaS gene deletion (ΔpdtaS) mutant shows increased sensitivity to Sisomicin sulfate (2.3μg/ml; 3, 6, 9 and 24h)[2]. Sisomicin sulfate (20μg/mL; 30min) does not interfere with the function of polymorphonuclear neutrophils (PMN)[3].

In vivo, Hypertonic Sisomicin sulfate (20mg/ml) can be used for intracochlear perfusion to construct an inner ear injury model in mice[4]. Sisomicin sulfate (20mg/kg; i.p.) caused a decrease in neuromuscular twitch tension in rabbits[5].

References:
[1] Noone P. Sisomicin sulfate, netilmicin and dibekacin. A review of their antibacterial activity and therapeutic use. Drugs. 1984 Jun;27(6):548-78.
[2] Dadura K, Płocińska R, Rumijowska-Galewicz A, et al. PdtaS Deficiency Affects Resistance of Mycobacteria to Ribosome Targeting Antibiotics. Front Microbiol. 2017 Nov 3;8:2145.
[3] Le Moli S, Seminara R, D'Amelio R, et al. In vitro and in vivo effect of Sisomicin sulfate and gentamycin on polymorphonuclear chemotaxis and phagocytosis. Int J Immunopharmacol. 1983;5(1):49-54.
[4] Maraslioglu-Sperber A, Blanc F, Heller S, et al. Hyperosmotic Sisomicin sulfate infusion: a mouse model for hearing loss. Sci Rep. 2024 Jul 10;14(1):15903.
[5] Matsukawa S, Suh JH, Hashimoto Y, et al. Neuromuscular blocking actions of the aminoglycoside antibiotics Sisomicin sulfate and micronomicin in the rabbit. Tohoku J Exp Med. 1997 Apr;181(4):471-3.

Sisomicin sulfate是一种由伊诺单孢菌(Micromonospora inyoensis)产生的天然氨基糖苷类抗生素,对革兰氏阳性菌具有很强的活性[1]

在体外实验中,与野生型分枝杆菌(Mycobacterium smegmatis)相比,PdtaS基因敲除(ΔpdtaS)突变株对Sisomicin sulfate(2.3µg/ml; 3, 6, 9和24h)的敏感性增加[2]。Sisomicin sulfate (20μg/mL; 30min) 不会干扰多形核中性粒细胞(PMN) 功能[3]

在体内实验中,高渗Sisomicin sulfate(20mg/ml; 耳内灌注)可用于构建小鼠内耳损伤模型[4]。Sisomicin sulfate(20mg/kg; i.p.)导致兔子神经肌肉抽搐张力降低[5]

实验参考方法

Cell experiment [1]:

Cell lines

Mycobacterium smegmatis

Preparation Method

The survival of M. smegmatis ΔpdtaS mutant cells grown in liquid medium with the addition of selected antibiotics was studied using standard colony-forming unit (CFU) methodology. Actively growing cells from the logarithmic stage of growth were diluted in 7H9 medium supplemented with OADC and Tween-80 to an OD600 of 0.1. Sisomicin sulfate at a final concentration of 2.3μg/ml was used. The kinetics of growth was measured by recording OD600 at 3, 6, 9 and 24h after the addition of antibiotics. At the 9 and 24h time points, 10-fold serial dilutions of cells were spread on 7H10 agar containing OADC. Plates were incubated at 37°C for 3-5 days, colonies were counted, and data were plotted using Excel. A Student's t-test was performed to determine the statistical significance between the test and control values.

Reaction Conditions

2.3μg/ml; 3, 6, 9 and 24h

Applications

Compared to the wild-type Mycobacterium smegmatis, the PdtaS gene deletion (ΔpdtaS) mutant shows increased sensitivity to Sisomicin sulfate.
Animal experiment [2]:

Animal models

Rabbits

Preparation Method

Twenty rabbits weighing 2.2-4.4kg were subjected to tracheotomy after anesthesia induction. Mechanical ventilation was controlled to maintain arterial carbon dioxide pressure (PaCO₂) between 35-45mmHg. Blood pressure and arterial blood gas analysis were monitored through a catheterized carotid artery. The external jugular vein was cannulated for fluid (5%D/W, at a rate of 10ml/kg/hr) and drug administration. The left gastrocnemius tendon was cut and secured to a U-type force-displacement transducer. A heating pad was used to maintain body temperature above 36°C, and the muscle was housed in a clear enclosure warmed by a heat lamp. A thermometer in contact with the muscle surface measured muscle temperature. The left tibial nerve was cut after dissection from the sciatic nerve and covered with mineral oil. The cut tibial nerve was directly stimulated using a stimulator and 27 gauge thin-walled steel-needle electrodes. Maximal square-wave pulses (0.1ms duration) were delivered at a rate of 0.1Hz. The resultant isometric force of muscle twitch tension and arterial blood pressure were continuously recorded on a Nihon Kohden polygraph.

When a stable twitch was obtained, an initial dose of Sisomicin sulfate (20mg/kg, n=7) was administered intravenously, and the initial dose and maximum percentage of twitch inhibition were determined. Additional Sisomicin sulfate (10mg/kg) was given to study the response to twitch inhibition exceeding 90%.

Dosage form

20mg/kg; i.p.

Applications

Sisomicin sulfate caused a decrease in neuromuscular twitch tension in rabbits.

References:
[1] Dadura K, P?oci?ska R, Rumijowska-Galewicz A, et al. PdtaS Deficiency Affects Resistance of Mycobacteria to Ribosome Targeting Antibiotics. Front Microbiol. 2017 Nov 3;8:2145.
[2] Matsukawa S, Suh JH, Hashimoto Y, et al. Neuromuscular blocking actions of the aminoglycoside antibiotics Sisomicin sulfate and micronomicin in the rabbit. Tohoku J Exp Med. 1997 Apr;181(4):471-3.

化学性质

Cas No. 53179-09-2 SDF
别名 硫酸西索米星
Canonical SMILES N[C@H]1[C@](O[C@@H]2[C@@H](N)C[C@@H](N)[C@H](O[C@@]3([H])OC[C@@](O)(C)[C@H](NC)[C@H]3O)[C@H]2O)([H])OC(CN)=CC1.[2.5H2SO4]
分子式 C19H37N5O7 . 5/2 H2SO4 分子量 692.72
溶解度 Water : 20 mg/mL (28.87 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.4436 mL 7.2179 mL 14.4358 mL
5 mM 288.7 μL 1.4436 mL 2.8872 mL
10 mM 144.4 μL 721.8 μL 1.4436 mL
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