Cefotaxime (sodium salt)
(Synonyms: 头孢噻肟钠 ; Cefotaxim sodium; HR-756 sodium) 目录号 : GC16544
Cefotaxime (sodium salt)是第三代头孢菌素，对广泛的革兰氏阳性菌和革兰氏阴性菌均有效。Cefotaxime可同时抑制酪氨酸酶的单酚酶和二酚酶活性，IC50值分别为3.2mM和0.14mM。
Cas No.:64485-93-4
Sample solution is provided at 25 µL, 10mM.
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Cefotaxime (sodium salt) is a third-generation cephalosporins against a wide range of gram positive and gram negative organisms[1]. Cefotaxime inhibits both the monophenolase and diphenolase activities of tyrosinase with IC50 values of 3.2mM and 0.14mM, respectively[2]. Cefotaxime is effective in the treatment of various infections: complicated urinary tract infections, lower respiratory tract infections, bacteraemia, meningitis, uncomplicated gonorrhoea, infections of skin and soft tissue and of bone and joints, and obstetric and gynaecological infections[3].
In vitro, Cefotaxime (100μg/ml) treatment for 72h specifically promoted the apoptosis in nasopharyngeal carcinoma CNE2 cells treated by cisplatin (2μg/ml). Cefotaxime (200μg/ml) treatment combined with cisplatin (2μg/ml) for 48h on CNE2 cells significantly regulated 5 genes in direction favoring the enhancement of anticancer efficacy; of which, THBS1 and LAPTM5 were upregulated; PPP3CB, STAG1 and NCOA5 were downregulated jointly[4]. Cefotaxime (0.25, 0.5 and 1mg/mL) incubation for 24 or 48h after 1mg/mL LPS stimulation boosted IL-2 production from mononuclear cells (MC) isolated from cord blood (CBMC) of newborns and from peripheral venous blood (PBMC) of adults. Cefotaxime also induced dose-dependent inhibition of the spontaneous and LPS induced IL-1β production, but had no effect on the production of IL-6 by cells of the two groups[5].
In vivo, Cefotaxime (30mg/kg; i.p.) and Ciprofloxacin (8mg/kg; i.p.) were injected into V. vulnificus. infected female BALB/c mice every 6h or 12h respectively for total 42h. Cefotaxime failed to effectively clear V. vulnificus in vivo but the combination of Ciprofloxacin and Cefotaxime significantly increased 96h survival rate from 0% to 85%[6]. Sub-inhibitory concentration of Cefotaxime (0.065mg/L (0.5× MIC)) applied to pretreated bacteria. S. Typhimurium for 3 hours increased the systemic colonization of S. Typhimurium in BALB/c mice after intraperitoneal inoculation in part by the establishment of a fitness alteration conducive to anaerobic metabolism[7].
References:
[1] Woodfield J C, Van Rij A M, Pettigrew R A, et al. A comparison of the prophylactic efficacy of ceftriaxone and cefotaxime in abdominal surgery.Am J Surg. 2003 Jan;185(1):45-9.
[2] Hu Y H, Zhuang J X, Yu F, et al. Inhibitory effects of cefotaxime on the activity of mushroom tyrosinase. J Biosci Bioeng. 2016 Apr;121(4):385-9.
[3] Todd P A, Brogden R N. Cefotaxime. An update of its pharmacology and therapeutic use. Drugs. 1990 Oct;40(4):608-51.
[4] He X Q, Yao Q, Fan D, et al. Combination of Cefotaxime and Cisplatin Specifically and Selectively Enhances Anticancer Efficacy in Nasopharyngeal Carcinoma.Curr Cancer Drug Targets. 2023;23(7):572-584.
[5] Bessler H, Gurary N, Aloni D, Vishne T H, Sirota L. Effect of cefotaxime on cytokine production in newborns and adults in vitro. Biomed Pharmacother. 2000 Aug;54(7):410-4.
[6] Jang H C, Choi S M, Kim H K, et al. In vivo efficacy of the combination of ciprofloxacin and cefotaxime against Vibrio vulnificus sepsis. PLoS One. 2014 Jun 30;9(6):e101118.
[7] Molina-Quiroz R C, Silva C A, Molina C F, et al. Exposure to sub-inhibitory concentrations of cefotaxime enhances the systemic colonization of Salmonella Typhimurium in BALB/c mice. Open Biol. 2015 Oct;5(10):150070.
Cefotaxime (sodium salt)是第三代头孢菌素，对广泛的革兰氏阳性菌和革兰氏阴性菌均有效[1]。Cefotaxime可同时抑制酪氨酸酶的单酚酶和二酚酶活性，IC50值分别为3.2mM和0.14mM[2]。Cefotaxime适用于多种感染的治疗：复杂性尿路感染、下呼吸道感染、败血症、脑膜炎、单纯性淋病、皮肤及软组织感染、骨关节感染以及妇产科感染[3]。
在体外实验中，Cefotaxime（100μg/ml）处理72小时可特异性促进cisplatin（2μg/ml）诱导的鼻咽癌CNE2细胞的凋亡。Cefotaxime（200μg/ml）联合cisplatin（2μg/ml）处理CNE2细胞48小时，显著调控了5个基因，增强抗癌效果；其中THBS1和LAPTM5表达上调，PPP3CB、STAG1和NCOA5共同下调[4]。Cefotaxime（0.25、0.5和1mg/mL）在1mg/mL LPS刺激后的24或48小时内孵育，可促进从新生儿脐带血（CBMC）和成人外周静脉血（PBMC）中分离出的单核细胞（MC）产生IL-2。Cefotaxime还诱导了对自发和LPS诱导的IL-1β产生的剂量依赖性抑制，但对两组细胞产生的IL-6无影响[5]。
在体内实验中，Cefotaxime（30mg/kg）和Ciprofloxacin（8mg/kg）分别每6小时或12小时向感染V.vulnificus的雌性BALB/c小鼠进行腹腔注射，总共42小时。Cefotaxime在体内未能有效清除V. vulnificus，但Ciprofloxacin与Cefotaxime的组合显著提高了96小时生存率，从Cefotaxime单独注射组的0%提高到85%[6]。Cefotaxime的亚抑制浓度（0.065mg/L（0.5× MIC））被应用于预先处理的沙门氏菌S.Typhimurium 3小时。Cefotaxime暴露通过建立了有利于厌氧代谢的适应性改变增加了BALB/c小鼠腹腔接种后S.Typhimurium的系统定植[7]。
| Cell experiment [1]: | |
Cell lines | Mononuclear cells (MC) |
Preparation Method | MC were incubated without or with 1.0mg/mL lipopolysaccharide for spontaneous and LPS-induced secretion of IL- 1β, with LPS for IL-6 and TNFα production and with 1% phytohemagglutinin for IL-2 production. Cefotaxime was added at the onset of the cultures at the following concentrations, 0.25, 0.5 and 1mg/mL. Culture media were collected at 24h (for IL- 1β, IL-6 and TNFα), or at 48h for IL-2. |
Reaction Conditions | 0.25, 0.5 and 1mg/mL; 24 and 48h |
Applications | Cefotaxime stimulated the production of IL-2 by cells of both adults and neonates, increased secretion of TNFα by PBMC of adults, but did not alter the synthesis of this cytokine by cord blood mononuclear cells of the newborns. Cefotaxime also induced dose-dependent inhibition of the spontaneous and LPS induced IL-1β production, but had no effect on theproduction of IL-6 by cells of the two groups. |
| Animal experiment [2]: | |
Animal models | Female BALB/c mice |
Preparation Method | Female BALB/c mice were injected subcutaneously with V. vulnificus. Cefotaxime (30mg/kg; i.p.) was initially given 2h after the animal was infected then every 6h for total 42h. Ciprofloxacin (8mg/kg; i.p.) was given every 12h. |
Dosage form | 30mg/kg; i.p.; every 6h for total 42h |
Applications | Cefotaxime failed to effectively clear V. vulnificus but the combination of Ciprofloxacin and Cefotaxime significantly increased 96h survival rate from 0% to 85%. |
References: | |
| Cas No. | 64485-93-4 | SDF | |
| 别名 | 头孢噻肟钠 ; Cefotaxim sodium; HR-756 sodium | ||
| 化学名 | (6R)-3-[(acetyloxy)methyl]-7R-[[(2Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, monosodium salt | ||
| Canonical SMILES | [H][C@@]1([C@@H]2NC(/C(C3=CSC(N)=N3)=N\OC)=O)N(C(C([O-])=O)=C(COC(C)=O)CS1)C2=O.[Na+] | ||
| 分子式 | C16H16N5O7S2 • Na | 分子量 | 477.5 |
| 溶解度 | ≥ 18.8mg/mL in DMSO | 储存条件 | Store at -20°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 | 2.0942 mL | 10.4712 mL | 20.9424 mL |
| 5 mM | 0.4188 mL | 2.0942 mL | 4.1885 mL |
| 10 mM | 0.2094 mL | 1.0471 mL | 2.0942 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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