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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。

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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

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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.

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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

依帕司他

依帕司他用途

依帕司他名称

依帕司他生物活性

依帕司他物理化学性质

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

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

依帕司他安全信息

依帕司他制备

依帕司他文献

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