非达司他

非达司他用途

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。

非达司他名称

[ CAS 号 ]:
136087-85-9

[ 中文名 ]:
非达司他

[ 英文名 ]:
Fidarestat

[中文别名 ]:

[英文别名 ]:

SNK-860
Fidarestat
Aldos
Sk 860

非达司他生物活性

[ 描述 ]:

[ 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.

[相关活性小分子]

非达司他物理化学性质

[ 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

非达司他毒性和生态

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