< 生产厂家 价格 >

西拉普利

西拉普利用途

Cilazapril一水合物是血管紧张素转化酶抑制剂,可作用于高血压和充血性心力衰竭。
点击显示

西拉普利名称

[ CAS 号 ]:
92077-78-6

[ 中文名 ]:
西拉普利

[ 英文名 ]:
Cilazapril (monohydrate)

[英文别名 ]:

西拉普利生物活性

[ 描述 ]:

Cilazapril一水合物是血管紧张素转化酶抑制剂,可作用于高血压和充血性心力衰竭。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 血管紧张素转换酶(ACE)
研究领域 >> 心血管疾病

[溶解度]

体外:

在DMSO中10mM


[储备液]

1 mM 2.2962 mL 11.4808 mL 22.9616 mL
5 mM 0.4592 mL 2.2962 mL 4.5923 mL
10 mM 0.2296 mL 1.1481 mL 2.2962 mL

[存储]

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月

[运输]

室温;可能会有所不同

[SMILES]

O=C([C@@H]1CCCN2N1C([C@@H](N[C@H](C(OCC)=O)CCC3=CC=CC=C3)CCC2)=O)O.O

[参考文献]

[1]. Szucs, T., Cilazapril. A review. Drugs, 1991. 41 Suppl 1: p. 18-24.

[2]. Nussberger, J., et al., Repeated administration of the converting enzyme inhibitor cilazapril to normal volunteers. J Cardiovasc Pharmacol, 1987. 9(1): p. 39-44.


[相关活性小分子]

血管紧张素1-7 | 卡托普利 | 马来酸依那普利 | 培哚普利 | 赖诺普利 | Phosphoramidon Disodium | 群多普利 | 福辛普利钠 | 盐酸喹那普利 | 雷米普利 | 依那普利那二水 | 奥马曲拉 | 盐酸替莫普利 | 西拉普利 | 血啡-7

[相关文档]

*以上文档由Medchemexpress提供,仅用于科学研究参考。

西拉普利物理化学性质

[ 沸点 ]:
598.1ºC at 760mmHg

[ 熔点 ]:
98° (dec)

[ 分子式 ]:
C22H33N3O6

[ 分子量 ]:
435.51400

[ 闪点 ]:
315.5ºC

[ 精确质量 ]:
435.23700

[ PSA ]:
108.41000

[ LogP ]:
1.79790

西拉普利毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UR6113250
CHEMICAL NAME :
6H-Pyridazino(1,2-a)(1,2)diazepine-1-carboxylic acid, octahydro-9-((1-(ethoxycarbonyl)-3- phenylpropyl)amino)-10-oxo-, hydrate, (1S-(1-alpha,9-alpha(R*)))-
CAS REGISTRY NUMBER :
92077-78-6
LAST UPDATED :
199706
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C22-H31-N3-O5.H2-O
MOLECULAR WEIGHT :
435.58

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
15 mg/kg/22W-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 345,398,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - hypermotility, diarrhea
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: 17,1281,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
830 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure) Behavioral - rigidity (including catalepsy)
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: 17,1281,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>30 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 17,1281,1989
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
5 gm/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Nutritional and Gross Metabolic - body temperature decrease
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: 17,1281,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair
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: 17,1281,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>30 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 17,1281,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,1,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
22750 mg/kg/13W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Blood - normocytic anemia Nutritional and Gross Metabolic - weight loss or decreased weight gain
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: 17,1295,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
22500 mg/kg/90D-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in erythrocyte (RBC) 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: 17,1333,1989
点击显示

西拉普利制备

化合物(Ⅱ)(24.6g,7.7mmo1)溶于135ml甲苯,在10℃和搅拌下,加入20.2g碳酸氢钠在200ml水的溶液,再加入酰氯(I)(从其酸(33.8g,90mmo1)和13.1rnl氯化亚砜在甲苯中反应制得)在150ml甲苯的溶液,然后在室温下搅拌17h,分层,有机层用Florisil柱层析。蒸去洗脱液,剩余物为化合物(Ⅲ),将其溶于500ml二甲基甲酰胺,加入5%钯-炭,氢化18h。滤去催化剂,滤液浓缩。剩余物用.50ml乙醚处理后,过滤。在10℃和搅拌下,将得到的白色固体溶于590ml二氯甲烷。在1.5min中,加入氯化亚砜(5.5ml,0.08mo1),再在室温下搅拌4h。加入15.5g碳酸氢钾在155ml水的溶液。分出有机层,浓缩,剩余物经层析得25.1g化合物(Ⅳ),收率76%,熔点188~189℃(乙酸乙酯-己烷),[α]D20-85.1°(C=0.5,甲醇)。
化合物(Ⅳ)(36.5g,85mmo1)溶于85ml干燥四氢呋喃中,在冷却、搅拌和缓慢氮气流下,加入1mol/L硼烷的四氢呋喃溶液(75.2ml,75mmo1),控制内温在10~15℃,约1h加毕。在10~15℃下搅拌1h,再在室温下搅拌3h。加入170ml二氯甲烷,再在搅拌下加入170ml 2mol/L盐酸。搅拌1.5min后,加入无水碳酸钠碱化。分出有机层,用盐水洗,浓缩。得31.7g化合物(V),收率90%,熔点140.5~141.5℃(含水乙醇),[α]D20-68.5°(C=1,甲醇)。
化合物(V)(8.26g,20mmo1)悬浮于82.6ml乙醇,加入水合肼(2.2g,44mmo1),在室温下搅拌1h。蒸出溶剂,剩余物加入甲苯,再蒸干。加入82.6ml 2mol/L乙酸水溶液,搅拌16h。过滤,滤液用无水碳酸钠碱化后,用二氯甲烷提取。提取液加入40ml。10%碳酸钠溶液,再在室温和搅拌下,加入(2R)-2-三氟甲磺酰氧基-4-苯基丁酸乙酯(Ⅵ)(7.48g,22mmo1)在20ml二氯甲烷的溶液,继续搅拌5h。分出有机层,和10g Florisil(商品名,即硅酸镁载体)一起搅拌30min,,过滤,滤液含化合物(Ⅶ),将其冷至0~5℃在搅拌下,通2h干燥的氯化氢气体。然后在室温下搅拌16h。浓缩,剩余物在水和乙醚之间进行分配。分出乙醚层,用1mol/L盐酸提取。提取液和水层合并,用5mol/L氢氧化钠溶液调至Ph=4.4。滤集固体,得7.21g西拉普利,收率83%。用二氯甲烷提取滤液,可得0.72g第二份西拉普利产品,收率8%。用含水乙醇重结晶后,熔点95~97℃,[α]D20-62.5°(C=1,乙醇)。

点击显示

西拉普利文献

Cilazapril stability in the presence of hydrochlorothiazide in model mixtures and fixed dose combination.

Acta Pol. Pharm. 70(6) , 1079-85, (2013)

The presented study aimed at the evaluation of hydrochlorothiazide influence on cilazapril stability in model mixture and fixed dose tablet formulation. The degradation of cilazapril in the presence o...

Common medications among dental outpatients: considerations in general dental practice.

N. Z. Dent. J. 108(4) , 140-7, (2012)

To provide information about the most common medications listed as being taken by dental patients presenting to an outpatient setting at a tertiary institution and to establish a list of the most comm...

Ultra-thin-layer chromatography mass spectrometry and thin-layer chromatography mass spectrometry of single peptides of angiotensin-converting enzyme inhibitors.

J. Chromatogr. A. 1218(20) , 3089-94, (2011)

The separation of structurally related angiotensin-converting enzyme (ACE) inhibitors lisinopril, cilazapril, ramipril and quinapril and their corresponding active diacid forms (prilates) by conventio...


更多文献

相关药品:

推荐生产厂家/供应商:

公司名:爱必信(上海)生物科技有限公司

区域:上海市浦东新区

价格:
¥1657.0/10mg ¥11601.0/100mg

联系人:周女士

产品详情:Cilazapril Monohydrate


公司名:MedChemExpress LLC

区域:上海市浦东新区

价格:
¥3348.0/50mg ¥837.0/10mg ¥5859.0/100mg

联系人:高小姐

产品详情:Cilazapril (monohydrate)


查看所有供应商请点击:

西拉普利供应商


相关化合物

【西拉普利】化源网提供西拉普利CAS号92077-78-6,西拉普利MSDS及其说明、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。CAS号查询西拉普利上化源网,专业又轻松。>>电脑版:西拉普利

标题:西拉普利_用途_熔点_沸点_西拉普利CAS号【92077-78-6】_化源网 地址:https://m.chemsrc.com/mip/cas/92077-78-6_843427.html