1492-02-0

• 常用中文名：格列丁唑
• 常用英文名：Glybuzole
• CAS号：1492-02-0
• 分子式：C₁₂H₁₅N₃O₂S₂
• 分子量：297.39600
• 相关类别： 研究领域 代谢疾病
• 发布时间：2018-08-09 20:35:34
• 更新时间：2024-01-13 19:34:19
• 格列苯唑(去糖基苯唑)是一种口服活性降糖药,具有抗糖尿病作用[1]。

名称

• 中文名: 格列丁唑
• 英文名: N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide
• 中文别名: N-(5-叔丁基-1,3,4-噻二唑-2-基)苯磺酰胺
• 英文别名: Gludiase; Glybuzolum [INN-Latin]; glybuzole; EINECS 216-081-2; Desaglybuzol; Glybuzole [INN:JAN]; AN 1324; sulfamidothiodiazol; N-(5-tert-butyl-1,3,4-thiadiazol-2-yl) benzenesulfonamide; RP 7891; Glibuzol [INN-Spanish]; Desaglybuzole; 2-Benzolsulfonamino-5-tert.-butyl-1,3,4-thiadiazol

物化性质

• 密度: 1.344g/cm3
• 沸点: 449.4ºC at 760mmHg
• 分子式: C₁₂H₁₅N₃O₂S₂
• 分子量: 297.39600
• 闪点: 225.6ºC
• 精确质量: 297.06100
• PSA: 108.57000
• LogP: 3.79020
• 蒸汽压: 2.88E-08mmHg at 25°C
• 折射率: 1.605

生物活性

• 描述: 格列苯唑(去糖基苯唑)是一种口服活性降糖药,具有抗糖尿病作用[1]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
• 体内研究: 格列苯唑(100 mg/kg,p.o.)很快被吸收,在狗和大鼠的血清中发现浓度为100-250 mg/L[1]。动物模型：狗或大鼠[1]剂量：100 mg/kg给药：口服(p.o.)结果：快速吸收,在血清中浓度为100-250 mg/L。在最初的几个小时内,48小时内的尿液排泄量为给药剂量的15-30%。
• 参考文献:

  [1]. Populaire P, Terlain B, Lebreton G, et al. Absorption, excretion and biotransformation of benzene sulfonamido-2-tertiobutyl-5-thiadiazole-1, 3, 4 (desaglybuzole= 7 891 RP). Therapie, 1969, 24(2): 313-326.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DB1290000 CHEMICAL NAME : Benzenesulfonamide, N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)- CAS REGISTRY NUMBER : 1492-02-0 LAST UPDATED : 199612 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C12-H15-N3-O2-S2 MOLECULAR WEIGHT : 297.42 WISWESSER LINE NOTATION : T5NN DSJ CX1&1&1 EMSWR 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 : 500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 219 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 310 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 550 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - dyspnea Endocrine - hypoglycemia REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,131,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 235 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 248 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 193 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 967 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 300 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 118 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2100 mg/kg SEX/DURATION : female 7-13 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2100 mg/kg SEX/DURATION : female 7-13 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetal death REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1050 mg/kg SEX/DURATION : female 7-13 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969