41136-22-5

• 常用中文名：头孢替唑钠
• 常用英文名：Ceftezole sodium
• CAS号：41136-22-5
• 分子式：C₁₃H₁₂N₈NaO₄S₃+
• 分子量：462.462
• 相关类别： 原料药 抗生素类药物 头孢菌素类药
• 发布时间：2018-03-22 08:00:00
• 更新时间：2024-01-20 19:41:21
• Ceftezole sodium (CTZ sodium) 是一种广谱 cephem 抗生素,具有抑制多种革兰氏阳性菌和革兰氏阴性菌活性。Ceftezole sodium (CTZ sodium) 是一种有效的 alpha-glucosidase 抑制剂,具有体内抗糖尿病活性。

名称

• 中文名: 头孢替唑钠
• 英文名: sodium,(6R,7R)-8-oxo-7-[[2-(tetrazol-1-yl)acetyl]amino]-3-(1,3,4-thiadiazol-2-ylsulfanylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
• 中文别名: (6R,7R)-3-[(1,3,4-噻二唑-2-基)硫代甲基]-8-氧代-7-[2-(1H-四唑-1-基)乙酰氨基]-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸钠; 头孢替坐钠
• 英文别名: Falomesin; MFCD01682031; ceftezole sodium; Celoslin; Alomen; Sodium (6R,7R)-8-oxo-7-[(1H-tetrazol-1-ylacetyl)amino]-3-[(1,3,4-thiadiazol-2-ylsulfanyl)methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 8-oxo-7-[[2-(1H-tetrazol-1-yl)acetyl]amino]-3-[(1,3,4-thiadiazol-2-ylthio)methyl]-, sodium salt, (6R,7R)- (1:1)

物化性质

• 密度: 2.09 g/cm3
• 分子式: C₁₃H₁₂N₈NaO₄S₃+
• 分子量: 462.462
• 精确质量: 461.996307
• PSA: 237.76000
• 外观性状: 粉末
• 储存条件: 库房低温通风干燥

生物活性

• 描述: Ceftezole sodium (CTZ sodium) 是一种广谱 cephem 抗生素,具有抑制多种革兰氏阳性菌和革兰氏阴性菌活性。Ceftezole sodium (CTZ sodium) 是一种有效的 alpha-glucosidase 抑制剂,具有体内抗糖尿病活性。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 参考文献:

  [1]. Lee DS, et al. Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity. Int J Mol Med. 2007 Sep;20(3):379-83.

  [2]. Harada Y, et al. Ceftezole, a new cephalosporin C derivative II. Distribution and excretion in parenteral administration. J Antibiot (Tokyo). 1976 Oct;29(10):1071-82.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : XI0400000 CHEMICAL NAME : 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 8-oxo-7-((1H-tetrazol-1-ylacetyl) amino)-3-((1,3,4-thiadiazol-2-ylthio)methyl)-, monosodium salt, (6R-trans)- CAS REGISTRY NUMBER : 41136-22-5 LAST UPDATED : 199606 DATA ITEMS CITED : 16 MOLECULAR FORMULA : C13-H11-N8-O4-S3.Na MOLECULAR WEIGHT : 462.49 WISWESSER LINE NOTATION : T46 ANV ES GUTJ HVO CMV1- AT5NNNNJ& G1S- CT5NN DSJ &-NA- HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >20 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - nausea or vomiting REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >11520 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >15 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Skin and Appendages - hair REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3800 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >15 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - nausea or vomiting REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 8900 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Skin and Appendages - hair REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 4700 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - nausea or vomiting REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >7 gm/kg TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - tremor REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 91 gm/kg/26W-I TOXIC EFFECTS : Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 6 gm/kg/30D-I TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in bladder weight Endocrine - changes in spleen weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 15 gm/kg/30D-I TOXIC EFFECTS : Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Skin and Appendages - dermatitis, other (after systemic exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 91 gm/kg/26W-I TOXIC EFFECTS : Blood - changes in bone marrow (not otherwise specified) Blood - changes in spleen Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 56400 mg/kg SEX/DURATION : male 26 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 24,671,1976