头孢美唑

头孢美唑用途

头孢美唑(CS 1170)是一种半合成的头孢霉素抗生素,具有广谱抗菌活性,包括革兰氏阳性菌、革兰氏阴性菌和厌氧菌。头孢美唑与青霉素结合蛋白(PBPs)结合,干扰细菌细胞壁生物合成。头孢美唑用于研究妇科、腹腔内、泌尿道、呼吸道以及皮肤和软组织感染[1][2][3]。

头孢美唑名称

[ CAS 号 ]:
56796-20-4

[ 中文名 ]:
头孢甲氧氰唑

[ 英文名 ]:
Cefmetazole

[中文别名 ]:

[英文别名 ]:

cefmetazolum [INN_la]
Cefmetazole
EINECS 260-384-2
MFCD00214260

头孢美唑生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体外研究]

头孢美唑(CS 1170)对金黄色葡萄球菌具有抗生素亲和力,MIC值为1.0mg/L。头孢美唑对PBP1、PBP2和PBP3具有亲和力,IC50值为≤0.3、0.109和0.494毫克/升[1]。

[体内研究]

头孢美唑(CS 1170)(100mg/kg；i.h.；每天两次,共7天；雄性ICR小鼠)改变肠道菌群[3]。动物模型：雄性ICR小鼠[3]剂量：100mg/kg给药：皮下注射；一天两次,持续7天。结果：减少派尔斑(PP)淋巴细胞数量,同时减少小肠细菌数量。

[参考文献]

[1]. Truesdell SE, et, al. Interaction of cephalosporins with penicillin-binding proteins of methicillin-resistant Staphylococcus aureus. J Antimicrob Chemother. 1989 Apr;23 Suppl D:13-9.

[2]. Schentag JJ. Cefmetazole sodium: pharmacology, pharmacokinetics, and clinical trials. Pharmacotherapy. 1991;11(1):2-19.

[3]. Yaguchi Y, et, al. Influences of long-term antibiotic administration on Peyer's patch lymphocytes and mucosal immunoglobulin A levels in a mouse model. JPEN J Parenter Enteral Nutr. 2006 Sep-Oct;30(5):395-8; discussion 399.

头孢美唑物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 熔点 ]:
163-165ºC

[ 分子式 ]:
C₁₅H₁₇N₇O₅S₃

[ 分子量 ]:
471.534

[ 精确质量 ]:
471.045319

[ PSA ]:
239.23000

[ LogP ]:
0.97

[ 外观性状 ]:
白色固体

[ 折射率 ]:
1.798

[ 储存条件 ]:
库房低温通风干燥

头孢美唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0372000

CHEMICAL NAME :: 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((((cyanomethyl)thio)acetyl)amino)- 7-methoxy-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl) -8-oxo-, (6R-cis)-

CAS REGISTRY NUMBER :: 56796-20-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C15-H17-N7-O5-S3

MOLECULAR WEIGHT :: 471.57

WISWESSER LINE NOTATION :: T46 ANV ES GUTJ CO1 CMV1S1CN HVQ G1S- ET5NNNNJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10233 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 31,49,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 12190 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 31,49,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8690 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 31,49,1979 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 9 gm/kg

SEX/DURATION :: female 18-35 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 6,289,1980

头孢美唑安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
XI0372200

头孢美唑合成路线

详细合成路线

头孢美唑文献

Long-Term Colonization by bla(CTX-M)-Harboring Escherichia coli in Healthy Japanese People Engaged in Food Handling.

Appl. Environ. Microbiol. 82 , 1818-27, (2016)

The actual state of intestinal long-term colonization by extended-spectrum β-lactamase (ESBL)-producing Escherichia coli in healthy Japanese people remains unclear. Therefore, a total of 4,314 fecal s...

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