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利尿酸

利尿酸用途

【用途一】
该品为强利尿药。具有抑制肾小管对钠、氯离子的再吸收作用，作用强而快，是严重水肿所必需的药物，但毒性较大，慢性肾功能不全者少用。鼠口服LD50为627mg/kg。

利尿酸名称

[ CAS 号 ]:
58-54-8

[ 中文名 ]:
利尿酸

[ 英文名 ]:
Ethacrynic acid

[中文别名 ]:

[英文别名 ]:

MFCD00056693
Ethacrynic Acid
EINECS 200-384-1

利尿酸生物活性

[ 描述 ]:

Ethacrynic acid 是一种利尿剂。Ethacrynic acid 是谷胱甘肽 S-转移酶 (GSTs) 的抑制剂。Ethacrynic acid 是一种 NF-κB 信号传导途径的有效抑制剂,并且还调节白三烯的形成。Ethacrynic acid 还可抑制 L 型电压依赖性和储存操作的钙通道,从而导致气道平滑肌细胞松弛。Ethacrynic acid 具有抗炎特性,可减轻类维生素 A 诱导的小鼠耳部水肿。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> 谷胱甘肽S-转移酶

研究领域 >> 炎症/免疫

[参考文献]

[1]. Li XQ, et al. Metabolism of Strained Rings: Glutathione S-transferase-Catalyzed Formation of a Glutathione-Conjugated Spiro-azetidine without Prior Bioactivation. Drug Metab Dispos. 2019 Nov;47(11):1247-1256.

[2]. Harada T, et al. Ethacrynic acid decreases expression of proinflammatory intestinal wall cytokines and ameliorates gastrointestinal stasis in murine postoperative ileus. Clinics (Sao Paulo). 2018 Oct 18;73:e332.

[3]. Zhao XX, et al. Ethacrynic acid inhibits airway smooth muscle contraction in mice. Sheng Li Xue Bao. 2019 Dec 25;71(6):863-873.

[4]. Byun HJ, et al. Ethacrynic Acid Inhibits Sphingosylphosphorylcholine-Induced Keratin 8 Phosphorylation and Reorganization via Transglutaminase-2 Inhibition. Biomol Ther (Seoul). 2013 Sep 30;21(5):338-42.

利尿酸物理化学性质

[ 密度 ]:
1.35g/cm3

[ 沸点 ]:
480ºC at 760mmHg

[ 熔点 ]:
125 °C

[ 分子式 ]:
C₁₃H₁₂Cl₂O₄

[ 分子量 ]:
303.13800

[ 闪点 ]:
244.1ºC

[ 精确质量 ]:
302.01100

[ PSA ]:
63.60000

[ LogP ]:
3.60570

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
-20?C Freezer

利尿酸MSDS

详细MSDS(安全技术说明书)

利尿酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG6600000

CHEMICAL NAME :: Acetic acid, (2,3-dichloro-4-(2-methylenebutyryl)phenoxy)-

CAS REGISTRY NUMBER :: 58-54-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C13-H12-Cl2-O4

MOLECULAR WEIGHT :: 303.15

WISWESSER LINE NOTATION :: QV1OR BG CG DVY2&U1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - change in acuity

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 117,715,1966

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - change in acuity Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 117,715,1966

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - tinnitus

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 117,715,1966

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1 gm/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,775,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 160 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 189 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 176 mg/kg

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

REFERENCE :: FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 23,438,1964

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0016635

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 449 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 78300 ug/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 469 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 14800 ug/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3792 No. of Facilities: 150 (estimated) No. of Industries: 2 No. of Occupations: 11 No. of Employees: 14149 (estimated) No. of Female Employees: 10194 (estimated)

利尿酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H312 + H332-H315-H319-H335

[ 警示性声明 ]:
P261-P280-P301 + P312 + P330-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
AG6600000

利尿酸合成路线

详细合成路线

利尿酸上下游产品

利尿酸上游产品

利尿酸下游产品

利尿酸制备

由2，3-二氯苯甲醚与丁酰氯缩合，并水解为2，3-二氯-4-丁酰苯酚，再与溴乙酸乙酯缩合，然后进一步与甲醛缩合并水解为依他尼酸。1.2，3-二氯-4-丁酰苯酚的制备将丁酰氯、二氯本甲醚及三氯化铝依次加入二硫化碳中，室温下反应1h，再加流1h后，回收二硫化碳。回收毕，加入正庚烷，再加入三氯化铝，继续回流3h。冷至50℃，分去正庚烷，冷却，加稀盐酸，升温至86℃，立即冷至40℃，过滤、洗涤，得2，3-二氯-4-丁酰苯酚粗品。粗品用酸碱法精制、活性炭脱色，得熔点为108-111℃的精品。收率85%。2.依他尼酸的制备将2，3-二氯-4-丁酰苯酚、无水乙醇和乙酸钠加热至回流，滴加溴乙酸乙酯，反应3h后回收乙醇。冷却，过滤，洗涤，用乙醇重结晶，得2，3-二氯-4-丁酰苯氧乙酸乙酯。然后将其投入甲醛和乙醇的混合液中，于回流下滴加碳酸钾、水和乙醇的混合液，继续回流1.5h。冷却，加稀盐酸析出沉淀，过滤、洗涤、干燥，最后经重结晶和活性炭脱色而得依他尼酸。收率约40%。

利尿酸文献

CYP2E1-mediated oxidative stress regulates HO-1 and GST expression in maneb- and paraquat-treated rat polymorphonuclear leukocytes.

Mol. Cell Biochem. 393(1-2) , 209-22, (2014)

Cytochrome P4502E1 (CYP2E1), glutathione-S-transferase A4-4 (GSTA4-4), and inducible nitric oxide synthase (iNOS) are implicated in maneb- and paraquat-induced toxicity leading to various pathological...

Purification and characterization of the Staphylococcus aureus bacillithiol transferase BstA.

Biochim. Biophys. Acta 1840(9) , 2851-61, (2014)

Gram-positive bacteria in the phylum Firmicutes synthesize the low molecular weight thiol bacillithiol rather than glutathione or mycothiol. The bacillithiol transferase YfiT from Bacillus subtilis wa...

Differential involvement of glutathione S-transferase mu 1 and multidrug resistance protein 1 in melanoma acquired resistance to vinca alkaloids.

Fundam. Clin. Pharmacol. 29(1) , 62-71, (2015)

On account of its extreme intrinsic resistance to apoptosis and of its strong ability to become chemoresistant after a primary response to drugs, malignant melanoma (MM) is still a therapeutic challen...

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利尿酸