2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯
用途
卡达拉嗪(ISF 2469)是一种口服活性抗高血压药物。卡达拉嗪是一种外周动脉血管扩张剂[1]。
名称
[ CAS 号 ]:
64241-34-5
[ 中文名 ]:
卡屈嗪
[ 英文名 ]:
Cadralazine
[中文别名 ]:
[英文别名 ]:
- DC-826
- Cadralazine [INN:BAN:JAN]
- Cadralazina [INN-Spanish]
- ISF 2469
- Cadralazine
- Cadralazina [Spanish]
- Cadralazinum [INN-Latin]
生物活性
物理化学性质
[ 密度 ]:
1.253 g/cm3
[ 沸点 ]:
425.88°C (rough estimate)
[ 熔点 ]:
160-162°
[ 分子式 ]:
C12H21N5O3
[ 分子量 ]:
283.32700
[ 精确质量 ]:
283.16400
[ PSA ]:
99.61000
[ LogP ]:
1.22060
[ 折射率 ]:
1.59
[ 储存条件 ]:
库房通风低温干燥
毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- MV1720400
- CHEMICAL NAME :
- Hydrazinecarboxylic acid, 2-(6-(ethyl(2-hydroxypropyl)amino)-3-pyridazinyl)-, ethyl ester
- CAS REGISTRY NUMBER :
- 64241-34-5
- BEILSTEIN REFERENCE NO. :
- 0894631
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 15
- MOLECULAR FORMULA :
- C12-H21-N5-O3
- MOLECULAR WEIGHT :
- 283.38
- WISWESSER LINE NOTATION :
- T6NNJ CN2&1YQ1 FMMVO2
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 :
- 2060 mg/kg
- TOXIC EFFECTS :
- Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section
- REFERENCE :
- JCPCDT Journal of Cardiovascular Pharmacology. (Raven Press, 1140 Ave. of the Americas, New York, NY 10036) V.1- 1979- Volume(issue)/page/year: 3,455,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 440 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,382,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Liver - other changes
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3839,1987
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 269 mg/kg
- TOXIC EFFECTS :
- Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section
- REFERENCE :
- JCPCDT Journal of Cardiovascular Pharmacology. (Raven Press, 1140 Ave. of the Americas, New York, NY 10036) V.1- 1979- Volume(issue)/page/year: 3,455,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 825 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,382,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 362 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,382,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1420 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - dyspnea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3839,1987
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 162 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,382,1982
- 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 :
- DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,382,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 400 mg/kg
- TOXIC EFFECTS :
- Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section Kidney, Ureter, Bladder - changes in blood vessels or in circulation of kidney
- REFERENCE :
- JCPCDT Journal of Cardiovascular Pharmacology. (Raven Press, 1140 Ave. of the Americas, New York, NY 10036) V.1- 1979- Volume(issue)/page/year: 3,455,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 36400 mg/kg/52W-C
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in spleen weight Blood - changes in leukocyte (WBC) count
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3875,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 9 gm/kg/30D-C
- TOXIC EFFECTS :
- Liver - changes in liver weight Endocrine - changes in spleen weight Blood - normocytic anemia
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3847,1987 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 132 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3913,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 3300 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3913,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 910 mg/kg
- SEX/DURATION :
- female 17-21 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,3945,1987
合成路线
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制备
在约70℃时，6h内往1L N-乙基-2-羟基丙胺中，加入583g 3，6-二氯酞嗪，在95℃下搅拌16h。然后加入1.5 L水、470ml 37%盐酸和884ml肼基甲酸乙酯，回流20h。用液氨调反应液的Ph值为8.5，得776g卡屈嗪。
推荐生产厂家/供应商：
公司名：上海化源世纪贸易有限公司
区域：上海市普陀区
价格：
联系人：徐乾明
产品详情：2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯
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：Cadralazine
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：
￥1743.9/100mg
￥350.9/10mg
￥4119.9/250mg
￥1647.9/50mg
联系人：阿拉丁
产品详情：卡达拉嗪
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CAS号[64241-34-5]化源网提供[2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯]MSDS、说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。>>电脑版：2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯
标题：64241-34-5_CAS号:64241-34-5_2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯 - 化源网 地址：https://www.chemsrc.com/amp/cas/64241-34-5_831787.html