136087-85-9

• 常用中文名：非达司他
• 常用英文名：Fidarestat
• CAS号：136087-85-9
• 分子式：C₁₂H₁₀FN₃O₄
• 分子量：279.224
• 相关类别： 信号通路 代谢酶/蛋白酶 醛糖还原酶
• 发布时间：2018-05-21 08:00:00
• 更新时间：2024-01-06 21:32:11
• Fidarestat (SNK 860) 是一种醛糖还原酶 (aldose reductase) 抑制剂,对 aldose reductase,AKR1B10 和 V301L AKR1B10 的 IC50 值分别为 26 nM,33 μM 和 1.8 μM；Fidarestat (SNK 860) 具有治疗糖尿病的潜力。

名称

• 中文名: 非达司他
• 英文名: Fidarestat
• 中文别名: (2S,4S)-6-氟-2',5'-二氧代-螺[色满-4,4'-咪唑啉]-2-甲酰胺; (2S,4S)-2-氨基甲酰-6-氟-螺[苯并二氢吡喃-4,4'-咪唑啉]-2',5'-酮
• 英文别名: SNK-860; Fidarestat; (+)-(2S,4S)-6-Fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide; Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxamide,6-fluoro-2,3-dihydro-2',5'-dioxo-,(2S-cis); (2s,4s)-2-aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione; Spiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide, 6-fluoro-2,3-dihydro-2',5'-dioxo-, (2S,4S)-; (2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide; (2S,4S)-2,3-Dihydro-6-fluoro-2',5'-dioxospiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide; (+)-(2s,4s)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide; (2S,4S)-6-Fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide; (2S,4S)-6-FLUORO-2'',5''-DIOXOSPIRO(3,4-DIHYDRO-2H-1-BENZOPYRAN-4,4''-IMIDAZOLIDINE)-2-CARBOXAMIDE; Aldos; Sk 860

物化性质

• 密度: 1.6±0.1 g/cm3
• 分子式: C₁₂H₁₀FN₃O₄
• 分子量: 279.224
• 精确质量: 279.065521
• PSA: 110.52000
• LogP: -0.24
• 折射率: 1.657
• 储存条件: -20°C，密闭，干燥

生物活性

• 描述: Fidarestat (SNK 860) 是一种醛糖还原酶 (aldose reductase) 抑制剂,对 aldose reductase,AKR1B10 和 V301L AKR1B10 的 IC50 值分别为 26 nM,33 μM 和 1.8 μM；Fidarestat (SNK 860) 具有治疗糖尿病的潜力。
• 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
• 靶点:

  IC50: 26 nM (Aldose reductase), 33 μM (AKR1B10), 1.8 μM (V301L AKR1B10)[1]

• 体外研究: Fidarestat是醛糖还原酶的抑制剂,醛糖还原酶,AKR1B10和V301L AKR1B10的IC50分别为26 nM,33μM和1.8μM[1]。
• 体内研究: Fidarestat(SNK-860; 1或4 mg/kg.po,每日4周)降低糖尿病大鼠中山梨糖醇和果糖的浓度[2]。
• 参考文献:

  [1]. Ruiz FX, et al. X-ray structure of the V301L aldo-keto reductase 1B10 complexed with NADP(+) and the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity. Chem Biol Interact. 2013 Feb 25;202(1-3):178-85.

  [2]. Hotta N, et al. Effect of an aldose reductase inhibitor, SNK-860, on deficits in the electroretinogram of diabetic rats. Exp Physiol. 1995 Nov;80(6):981-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : WG9863500 CHEMICAL NAME : Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxami de, 2,3-dihydro-2',5'-dioxo-6-fluoro-, (2S-cis)- CAS REGISTRY NUMBER : 136087-85-9 LAST UPDATED : 199712 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C12-H10-F-N3-O4 MOLECULAR WEIGHT : 279.25 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 : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990