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甲苯磺酸妥苏沙星(T 3262)

甲苯磺酸妥苏沙星(T 3262)用途

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]。

甲苯磺酸妥苏沙星(T 3262)名称

[ CAS 号 ]:
115964-29-9

[ 中文名 ]:
甲苯磺酸妥舒沙星

[ 英文名 ]:
UNII:NO6NM634EH

[中文别名 ]:

[英文别名 ]:

甲苯磺酸妥苏沙星(T 3262)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.  

甲苯磺酸妥苏沙星(T 3262)物理化学性质

[ 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

甲苯磺酸妥苏沙星(T 3262)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

甲苯磺酸妥苏沙星(T 3262)安全信息

[ 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

相关药品：

推荐生产厂家/供应商：

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Tosufloxacin

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥684.0/500mg ￥1278.0/1g ￥351.0/100mg ￥需询单/1g

联系人：阿拉丁李高志

产品详情：甲苯磺酸妥苏沙星（T 3262）

公司名：武汉鼎信通药业有限公司

区域：武汉市江夏区

价格：
￥需询单/1kg $需询单/10kg $需询单/50kg $需询单/500kg

联系人：董浩

产品详情：甲苯磺酸妥舒沙星

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