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马洛替酯

马洛替酯用途

Malotilate可作用于肝细胞,促进其RNA合成,激活核糖体,提高蛋白质合成能力,从而激活肝功能并抑制肝纤维化,还能抑制肝内4-羟基脯氨酸量的增加。

马洛替酯名称

[ CAS 号 ]:
59937-28-9

[ 中文名 ]:
二噻茂醋

[ 英文名 ]:
Malotilate

[中文别名 ]:

[英文别名 ]:

马洛替酯生物活性

[ 描述 ]:

Malotilate可作用于肝细胞,促进其RNA合成,激活核糖体,提高蛋白质合成能力,从而激活肝功能并抑制肝纤维化,还能抑制肝内4-羟基脯氨酸量的增加。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 5脂氧合酶
研究领域 >> 癌症
天然产物 >> 其他

[参考文献]

[1]. Shibata T, et al. Inhibitory effects of malotilate on in vitro invasion of lung endothelial cell monolayer by human oral squamous cell carcinoma cells. Tumour Biol. 2000 Sep-Oct;21(5):299-308.

[2]. Takase S, et al. Effects of malotilate treatment on alcoholic liver disease. Alcohol. 1989 May-Jun;6(3):219-22.

[3]. Nagayasu H, et al. Inhibitory effects of malotilate on invasion and metastasis of rat mammary carcinoma cells by modifying the functions of vascular endothelial cells. Br J Cancer. 1998 May;77(9):1371-7.

[4]. Ryhanen L, et al. The effect of malotilate on type III and type IV collagen, laminin and fibronectin metabolism in dimethylnitrosamine-induced liver fibrosis in the rat. J Hepatol. 1996 Feb;24(2):238-45.

[5]. Nomura F, et al. Detection of malotilate toxicity in vitro with peripheral blood mononuclear cells as targets. A preliminary report. J Hepatol. 1990 Jul;11(1):65-9.


[相关活性小分子]

U型73122 | 齐留通 | ML355 | 去甲二氢愈创木酸 | 靛玉红-3'-单肟 | 咖啡酸 | 异紫花前胡内酯 | 5,4'-二羟基黄酮 | 依那扎群 | LY 178002 | RWJ 63556 | S-2474 | 1-ethyl-3-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-5,5-dimethyl-2-thioxoimidazolidin-4-one | N-1-(Fur-3-ylethyl)-N-hydroxyurea | AZD 4407

马洛替酯物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
321.5±42.0 °C at 760 mmHg

[ 分子式 ]:
C12H16O4S2

[ 分子量 ]:
288.383

[ 闪点 ]:
138.7±15.9 °C

[ 精确质量 ]:
288.049011

[ PSA ]:
103.20000

[ LogP ]:
3.83

[ 蒸汽压 ]:
0.0±0.7 mmHg at 25°C

[ 折射率 ]:
1.562

[ 储存条件 ]:
-20°C

马洛替酯MSDS

马洛替酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
OO0970000
CHEMICAL NAME :
Malonic acid, (1,3-dithiol-2-ylidene)-, diisopropyl ester
CAS REGISTRY NUMBER :
59937-28-9
LAST UPDATED :
199506
DATA ITEMS CITED :
21
MOLECULAR FORMULA :
C12-H16-O4-S2
MOLECULAR WEIGHT :
288.40
WISWESSER LINE NOTATION :
T45 ESYSTJ FUYVOY1&1&VOY1&1

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 :
2065 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3120 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1220 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1732 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
SYXUE3 Shenyang Yaoxueyuan Xuebao. Journal of Shenyang College of Pharmacy. (Shenyang Yaoxueyuan, 7, 2-duan, Wenhualu, Shenhequ, Shenyang, Peop. Rep. China) V.1- 1984- Volume(issue)/page/year: 2,269,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
729 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
SYXUE3 Shenyang Yaoxueyuan Xuebao. Journal of Shenyang College of Pharmacy. (Shenyang Yaoxueyuan, 7, 2-duan, Wenhualu, Shenhequ, Shenyang, Peop. Rep. China) V.1- 1984- Volume(issue)/page/year: 2,269,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
706 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
656 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
2101 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
1011 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - hamster
DOSE/DURATION :
2707 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - hamster
DOSE/DURATION :
1533 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 25,387,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
10500 mg/kg/5W-I
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in spleen weight Blood - normocytic anemia
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 8,131,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
28 gm/kg/4W-I
TOXIC EFFECTS :
Behavioral - food intake (animal) Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 8,155,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
182 gm/kg/52W-I
TOXIC EFFECTS :
Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 8,155,1982 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3200 mg/kg
SEX/DURATION :
female 8-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 28,859,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1920 mg/kg
SEX/DURATION :
female 7-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 28,880,1981

马洛替酯安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36/37/39

马洛替酯制备

将1,3-二噻茂-2-硫酮-4,5-二羧酸溶于硝基甲烷,加热,然后缓慢滴加碘甲烷,加毕继续回流,反应结束后,经处理得到2-甲硫基-1,3-二噻茂碘化物。将氢化钠悬浮于四氢呋喃中,在冰浴冷却下,缓慢滴加丙二酸二异丙酯,反应一定时间,滴加上面得到的碘化物,回流。将反应液放入大量的冰水中,过滤收集形成的结晶,干燥,用狀己烷重结晶,得到马洛替酯。

或者丙二酸二异丙酯和二硫化碳在二甲亚砜中、氢氧化钾存在下反应,得到的产物和1,1,1-三氯乙烷,在氢氧化钾作用下反应,得到马洛替酯。


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公司名:上海化源生化科技有限公司

区域:上海市普陀区

价格:

联系人:化源网

产品详情:2-(1,3-二硫杂环戊二烯-2-亚甲基)丙二酸二异丙酯


公司名:上海源溪生物科技有限公司

区域:上海市浦东新区

价格:
¥需询单/1g

联系人:赖经理

产品详情:Malotilate


公司名:上海脉铂医药科技有限公司

区域:上海市嘉定区

价格:
¥759.0/1g ¥1839.0/100mg ¥429.0/5mg ¥需询单/1g

联系人:李先生

产品详情:Malotilate


公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

价格:
¥335.9/1g ¥1048.9/1ml ¥1026.9/5g ¥需询单/1g

联系人:阿拉丁

产品详情:马洛替酯


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相关化合物

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