<生产厂家价格>

依帕司他

依帕司他用途

Epalrestat是醛糖还原酶抑制剂,可作用于糖尿病神经病变。

依帕司他名称

[ CAS 号 ]:
82159-09-9

[ 中文名 ]:
依帕司他

[ 英文名 ]:
Epalrestat

[中文别名 ]:

[英文别名 ]:

Epalrestat
Kinedak
Ono 2235

依帕司他生物活性

[ 描述 ]:

Epalrestat是醛糖还原酶抑制剂,可作用于糖尿病神经病变。

[ 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

[参考文献]

[1]. Ramirez, M.A. and N.L. Borja, Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy. Pharmacotherapy, 2008. 28(5): p. 646-55.

[2]. Okamoto, H., et al., Effects of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy and gastroparesis. Intern Med, 2003. 42(8): p. 655-64.

[3]. Hotta, N., et al., Clinical investigation of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy in Japan: multicenter study. Diabetic Neuropathy Study Group in Japan. J Diabetes Complications, 1996. 10(3): p. 168-72.

[相关活性小分子]

依帕司他物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
516.8±60.0 °C at 760 mmHg

[ 熔点 ]:
210-217ºC

[ 分子式 ]:
C₁₅H₁₃NO₃S₂

[ 分子量 ]:
319.399

[ 闪点 ]:
266.4±32.9 °C

[ 精确质量 ]:
319.033691

[ PSA ]:
115.00000

[ LogP ]:
2.02

[ 外观性状 ]:
yellow to orange

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.706

[ 储存条件 ]:
通风低温干燥,与库房食品原料分开存放

[ 水溶解性 ]:
DMSO: soluble5mg/mL, clear (warmed)

依帕司他MSDS

详细MSDS(安全技术说明书)

依帕司他毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ5131855

CHEMICAL NAME :: 3-Thiazolidineacetic acid, 5-(2-methyl-3-phenyl-2-propenylidene)-4-oxo-2-thioxo- , (E,E)-

CAS REGISTRY NUMBER :: 82159-09-9

LAST UPDATED :: 199209

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C15-H13-N-O3-S2

MOLECULAR WEIGHT :: 319.41

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 :: 5300 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 922 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 255 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 687 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 255 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,201,1992

依帕司他安全信息

[ 危险品运输编码 ]:
2811

[ RTECS号 ]:
XJ5131855

[ 包装等级 ]:
II

依帕司他制备

将苯甲醛、乙醇、氢氧化钠和水混合,滴加丙醛反应,经处理得2-甲基3-苯基丙烯醛.

将二硫化碳和二氧六环溶于浓氨水,搅拌下,滴加甘氨酸钠溶液,反应,蒸干后,加入氯乙酸钠溶液,室温反应,蒸干,加水和浓盐酸,沸水浴加热,生成物经重结晶,得3-羧甲基绕单宁.将3-羧甲基绕单宁、2-甲基-3-苯基丙烯醛、无水乙酸钠和冰乙酸一起回流,经处理得到依帕司他.

依帕司他文献

Inhibitor selectivity between aldo–keto reductase superfamily members AKR1B10 and AKR1B1: Role of Trp112 (Trp111)

FEBS Lett. 587(22) , 3681-6, (2013)

• Crystal structures of AKR1B10 holoenzyme. • Trp112 side-chain flipping in AKR1B10 explains non-selectivity of AKR1B1 inhibitors. • Native Trp112 side-chain orientation is critical for selective AKR1...

Docking and molecular dynamics studies toward the binding of new natural phenolic marine inhibitors and aldose reductase

J. Mol. Graph. Model. 28(2) , 162-9, (2009)

Phenolic marine natural product is a kind of new potential aldose reductase inhibitors (ARIs). In order to investigate the binding mode and inhibition mechanism, molecular docking and dynamics studies...

6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2.

Bioorg. Med. Chem. Lett. 20 , 5630-3, (2010)

We report the structure-activity relationship of a series of coumarins as aldose reductase 2 (ALR2) inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens. We evalua...

更多文献