115964-29-9

• 常用中文名：甲苯磺酸妥苏沙星(T 3262)
• 常用英文名：UNII:NO6NM634EH
• CAS号：115964-29-9
• 分子式：C₂₆H₂₃F₃N₄O₆S
• 分子量：576.54
• 相关类别： 原料药 人工合成抗感染类药 喹诺酮类药
• 发布时间：2018-04-30 08:00:00
• 更新时间：2024-01-11 22:00:20
• 甲苯磺酸托苏沙星(A-61827)是一种口服活性氟喹诺酮类抗生素。甲苯磺酸托苏沙星对革兰氏阳性菌和革兰氏阴性菌具有广谱抗菌活性[1][2]。

名称

• 中文名: 甲苯磺酸妥舒沙星
• 英文名: Tosufloxacin tosylate
• 中文别名: 7-(3-氨基吡咯烷-1-基)-1-(2,4-二氟苯基)-6-氟-4-氧代-1,8-萘啶-3-甲酸 4-甲基苯磺酸盐; 甲苯磺酸托氟沙星
• 英文别名: Tosuxacin; TOSUFLOXACIN P TOSYLATE; Tosufloxacin Toluenesulfonate Hydrate; TFLX p-Toluenesulfonate; t3262; 7-(3-Aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 4-methylbenzenesulfonate (1:1); Ozax; 7-(3-Amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 4-methylbenzenesulfonate (1:1); UNII:NO6NM634EH; 1,8-Naphthyridine-3-carboxylic acid, 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-, 4-methylbenzenesulfonate (1:1); Tosufloxacin p-Toluenesulfonate; Tosufloxacin p-Toluenesulfonate Hydrate

物化性质

• 密度: 1.558g/cm3
• 沸点: 614.4ºC at 760mmHg
• 熔点: 251-252ºC
• 分子式: C₂₆H₂₃F₃N₄O₆S
• 分子量: 576.54
• 精确质量: 576.129028
• PSA: 164.20000
• LogP: 5.12640
• 外观性状: 白色至灰白色固体
• 储存条件: Refrigerator

生物活性

• 描述: 甲苯磺酸托苏沙星(A-61827)是一种口服活性氟喹诺酮类抗生素。甲苯磺酸托苏沙星对革兰氏阳性菌和革兰氏阴性菌具有广谱抗菌活性[1][2]。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 体外研究: 甲苯磺酸托苏沙星水合物(T-3262)(0.05-3.13μg/mL；18小时)对金黄色葡萄球菌、表皮葡萄球菌、链球菌、肠球菌、脆弱拟杆菌、艰难梭菌和产气荚膜梭菌具有抗菌活性[2]。细胞活力测定[2]细胞系：金黄色葡萄球菌、表皮葡萄球菌、链球菌、肠球菌、脆弱拟杆菌、艰难梭菌和产气荚膜梭菌浓度：0.05-3.13μg/mL培养时间：18小时结果：金黄色葡球菌、表皮葡球菌、链球菌和肠球菌的MIC90(90%测试分离株的MIC)范围为0.05-1.56μg/mL。脆弱拟杆菌、艰难梭菌和产气荚膜梭菌的MIC90分别为1.56、3.13和0.20μg/mL。
• 体内研究: 甲苯磺酸托苏沙星水合物(T-3262)(经口灌胃；0.16-13.39 mg/kg；一次)治疗显示出对体内金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌的抗菌活性[2]。动物模型：感染金黄色葡萄球菌的雄性Slc:ICR小鼠[2]剂量：1.27-2.15 mg/kg给药：灌胃；1.27-2.15 mg/kg；1次结果：感染后7天显示50%有效剂量(ED50)为1.62mg/kg(体重)。MIC值为0.0125μg/mL。动物模型：感染大肠杆菌的雄性Slc:ICR小鼠[2]剂量：0.16-0.30 mg/kg给药：灌胃；0.16-0.30 mg/kg；1次结果：感染后第7天显示50%有效剂量(ED50)0.22mg/kg(体重)。MIC值为0.0125μg/mL。动物模型：感染铜绿假单胞菌的雄性Slc:ICR小鼠[2]剂量：7.66-13.39 mg/kg给药：灌胃；7.66-13.39 mg/kg；结果：感染后7天ED50为10.13mg/kg(体重),为50%有效剂量。MIC值为0.78μg/mL。
• 参考文献:

  [1]. Chu DT, et al. Synthesis and biological properties of A-71497: a prodrug of tosufloxacin. Drugs Exp Clin Res. 1990;16(9):435-43.

  [2]. Fujimaki K, et al. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827-33.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : QN2791000 CHEMICAL NAME : 1,8-Naphthyridine-3-carboxylic acid, 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)- 6-fluoro-1,4-dihydro-4-oxo-, mono(4-methylbenzenesulfonate) CAS REGISTRY NUMBER : 115964-29-9 LAST UPDATED : 199806 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C19-H15-F3-N4-O3.C7-H8-O3-S MOLECULAR WEIGHT : 576.59 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 : >6 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >6 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >6 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: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 270 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - respiratory depression REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >6 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >6 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >6 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: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 196 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea 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: 36(Suppl 9),221,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : 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: 36(Suppl 9),221,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 72800 mg/kg/26W-I TOXIC EFFECTS : Gastrointestinal - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Metabolism (Intermediary) - other proteins REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),233,1988 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 700 mg/kg/14D-I TOXIC EFFECTS : Cardiac - changes in heart weight Gastrointestinal - other changes Related to Chronic Data - changes in prostate weight REFERENCE : JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 42,800,1989 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 33 gm/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),294,1988 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2080 mg/kg SEX/DURATION : female 17 day(s) after conception - 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 36(Suppl 9),294,1988

安全

• 符号: GHS07
• 信号词: Warning
• 危害声明: H315-H319-H335
• 警示性声明: P261-P305 + P351 + P338
• 危害码 (欧洲): Xi
• 风险声明 (欧洲): 36/37/38
• 安全声明 (欧洲): 26-36
• 危险品运输编码: NONH for all modes of transport
• RTECS号: QN2791000
• 海关编码: 29339900