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Cefotaxime Sale

(Synonyms: 头孢噻肟酸,Cefotaxim; HR-756) 目录号 : GC60685

Cefotaxime是一种具有广谱抗菌活性的第三代头孢菌素类抗生素。它最常用于治疗革兰氏阳性菌或革兰氏阴性菌引起的传染病。

Cefotaxime Chemical Structure

Cas No.:63527-52-6

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10mM (in 1mL DMSO)
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100mg
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250mg
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500mg
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Sample solution is provided at 25 µL, 10mM.

Description

Cefotaxime is a third-generation cephalosporin antibiotic with broad-spectrum antibacterial activity. It is most commonly prescribed for the treatment of infectious diseases induced by Gram-positive or Gram-negative bacteria[1].

Cefotaxime (200, 400, 600, or 1000μg/mL; 24h) significantly promotes ROS generation in HT1080 cells[1]. Cefotaxime (0.02-2µg/ml, 5h) combined with Mecillinam could eliminate both cephalosporin-resistant bacteria harbouring CTX-M-15WT and mecillinam-resistant bacteria harbouring the mutant CTX-M-15N135D, thereby constraining resistance evolution of β-lactamase CTX-M-15[2].

Cefotaxime (200 or 400mg/kg/8h, 9 injections, subcutaneous injection) significantly increased bacterial clearance from the pneumonia model in leukopenic mice[3]. Cefotaxime (100mg/kg/4h, 24h, subcutaneous injections) combined with Amoxicillin-Clavulanate significantly reduces bacterial counts and achieves kidney sterilization in in a Murine Urinary Tract Infection Model[4].

References:
[1] Yamada M, Suzuki M, Noguchi T, et al. The antibiotic cefotaxime works as both an activator of Nrf2 and an inducer of HSP70 in mammalian cells. BPB reports. 2020;3(1):16-21.
[2] Rosenkilde CE, Munck C, Porse A, et al. Collateral sensitivity constrains resistance evolution of the CTX-M-15 β-lactamase. Nature communications. 2019 Feb 6;10(1):618.
[3] Sauve C, Azoulay-Dupuis E, Moine P, et al. Efficacies of cefotaxime and ceftriaxone in a mouse model of pneumonia induced by two penicillin-and cephalosporin-resistant strains of Streptococcus pneumoniae. Antimicrobial agents and chemotherapy. 1996 Dec;40(12):2829-34.
[4] Rossi B, Soubirou JF, Chau F, et al. Cefotaxime and amoxicillin-clavulanate synergism against extended-spectrum-β-lactamase-producing Escherichia coli in a murine model of urinary tract infection. Antimicrobial Agents and Chemotherapy. 2016 Jan;60(1):424-30.

Cefotaxime是一种具有广谱抗菌活性的第三代头孢菌素类抗生素。它最常用于治疗革兰氏阳性菌或革兰氏阴性菌引起的传染病[1]

Cefotaxime(200、400、600或1000μg/mL,24小时)显著促进HT1080细胞中的ROS生成[1]。Cefotaxime(0.02-2µg/ml,5h)与Mecillinam联合应用,可以同时消灭携带CTX-M-15WT的头孢菌素耐药菌和携带突变体CTX-M-15N135D的Mecillinam耐药菌,从而抑制β-内酰胺酶CTX-M-15的耐药性进化[2]

Cefotaxime(200或400mg/kg/8小时,9次注射,皮下注射)显著增加白细胞减少小鼠的肺炎模型中的细菌清除率[3]。Cefotaxime(100mg/kg/4h,24h,皮下注射)与Amoxicillin-Clavulanate联合使用,在小鼠尿路感染模型中显著降低细菌数量并实现肾脏消毒[4]

实验参考方法

Cell experiment [1]:

Cell lines

Human fibrosarcoma HT1080 cells

Preparation Method

HT1080 cells were seeded on glass plates and treated with the indicated concentrations (200, 400, 600, or 1000μg/mL) of Cefotaxime for 24h. After stimulation, cells were treated with 10µM DCFH-DA for 30min at 37°C. After washing with PBS, the intracellular ROS generation was observed under laser confocal microscope.

Reaction Conditions

200, 400, 600, or 1000μg/mL; 24h

Applications

Cefotaxime significantly promotes ROS generation in HT1080 cells.
Animal experiment [2]:

Animal models

Pneumonia model in leukopenic mice

Preparation Method

Amoxicillin (AMO) and Cefotaxime (CTX) were administered at 8-h intervals with a total of nine injections, and Ceftriaxone (CRO) was given at 12-h intervals with a total of six injections. The dose of each antibiotic varied with the infective strain. Mice infected with strain P40422 were treated with AMO or CTX at 200 or 400mg/kg or with CRO at 100mg/kg. Mice infected with P40984 were treated with AMO at 200 or 400mg/kg, CTX at 400mg/kg, or CRO at 100 or 200mg/kg. Each dose was administered subcutaneously (s.c.) in 0.5ml of sterile water. Control animals received the same volume of isotonic saline.

Dosage form

200 or 400mg/kg/8h, 9 injections, subcutaneous injection

Applications

Cefotaxime significantly increased bacterial clearance from the pneumonia model in leukopenic mice.

References:
[1] Yamada M, Suzuki M, Noguchi T, et al. The antibiotic cefotaxime works as both an activator of Nrf2 and an inducer of HSP70 in mammalian cells. BPB reports. 2020;3(1):16-21.
[2] Sauve C, Azoulay-Dupuis E, Moine P, et al. Efficacies of cefotaxime and ceftriaxone in a mouse model of pneumonia induced by two penicillin-and cephalosporin-resistant strains of Streptococcus pneumoniae. Antimicrobial agents and chemotherapy. 1996 Dec;40(12):2829-34.

化学性质

Cas No. 63527-52-6 SDF
别名 头孢噻肟酸,Cefotaxim; HR-756
Canonical SMILES O=C(C(N12)=C(COC(C)=O)CS[C@]2([H])[C@H](NC(/C(C3=CSC(N)=N3)=N\OC)=O)C1=O)O
分子式 C16H17N5O7S2 分子量 455.47
溶解度 DMSO: 250 mg/mL (548.88 mM) 储存条件 Store at 2-8°C
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1 mg 5 mg 10 mg
1 mM 2.1955 mL 10.9777 mL 21.9553 mL
5 mM 0.4391 mL 2.1955 mL 4.3911 mL
10 mM 0.2196 mL 1.0978 mL 2.1955 mL
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