89391-50-4

• 常用中文名：咪瑞司他
• 常用英文名：IMIRESTAT
• CAS号：89391-50-4
• 分子式：C₁₅H₈F₂N₂O₂
• 分子量：286.23300
• 相关类别： 信号通路 代谢酶/蛋白酶 醛糖还原酶
• 发布时间：2018-07-08 19:13:40
• 更新时间：2024-01-04 18:33:40
• Imirestat (AL 1576) 是一种 aldose reductase 抑制剂,可用于治疗糖尿病。

名称

• 中文名: 咪瑞司他
• 英文名: 2,7-difluorospiro[fluorene-9,5'-imidazolidine]-2',4'-dione
• 英文别名: Imirestatum [INN-Latin]; Alcon 1576; 2,7-Difluorospiro(fluorene-9,4'-imidazolidine)-2',5'-dione; 2,7-di-fluoro-spiro(9H-fluorene-9,4'-imidazolidine)-2',5'-dione; Imirestat; spiro-[2,7-difluorofluoren-9,4'-imidazolidine]-2',5'-dione; Spiro(9H-fluorene-9,4'-imidazolidine)-2',5'-dione,2,7-difluoro; [14C]-Imirestat; Spiro-(2,7-difluoro-9H-fluoren-9,4'-imidazolidine)-2',5'-dione; HOE 843

物化性质

• 密度: 1.58g/cm3
• 分子式: C₁₅H₈F₂N₂O₂
• 分子量: 286.23300
• 精确质量: 286.05500
• PSA: 58.20000
• LogP: 2.68580
• 折射率: 1.692
• 储存条件: 2-8℃

生物活性

• 描述: Imirestat (AL 1576) 是一种 aldose reductase 抑制剂,可用于治疗糖尿病。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 醛糖还原酶
  研究领域 >> 代谢疾病
• 体内研究: Imirestat(1 mg/kg)可改善神经传导速度,但不会影响对缺氧传导阻滞的抵抗或胰岛素刺激的对人体敏感的ATP酶活性的缺陷[1]。
• 参考文献:

  [1]. Carrington AL, et al. Aldose reductase inhibition with imirestat-effects on impulse conduction and insulin-stimulation of Na+/K(+)-adenosine triphosphatase activity in sciatic nerves of streptozotocin-diabetic rats. Diabetologia. 1991 Jun;34(6):397-401.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : WH1307300 CHEMICAL NAME : Spiro(9H-fluorene-9,4'-imidazolidine)-2',5'-dione, 2,7-difluoro- CAS REGISTRY NUMBER : 89391-50-4 LAST UPDATED : 199712 DATA ITEMS CITED : 2 MOLECULAR FORMULA : C15-H8-F2-N2-O2 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 700 mg/kg/14D-I TOXIC EFFECTS : Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),137,1997 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - hamster DOSE/DURATION : 700 mg/kg/14D-I TOXIC EFFECTS : Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 36(1, Pt 2),137,1997

合成路线

24313-53-9 ~% 89391-50-4

文献：Alcon Laboratories, Inc. Patent: US4436745 A1, 1984 ; Title/Abstract Full Text Show Details Alcon Laboratories, Inc. Patent: US4540700 A1, 1985 ;

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