111223-26-8

• 常用中文名：西罗普利
• 常用英文名：Ceronapril
• CAS号：111223-26-8
• 分子式：C₂₁H₃₃N₂O₆P
• 分子量：440.47000
• 相关类别： 信号通路 代谢酶/蛋白酶 血管紧张素转换酶(ACE)
• 发布时间：2018-10-04 19:12:23
• 更新时间：2024-01-04 09:33:31
• Ceronapril(SQ 29852)是一种有效的口服活性血管紧张素转换酶(ACE)抑制剂,IC50为36 nM[1]。

名称

• 中文名: 西罗普利
• 英文名: 1-[6-amino-2-[hydroxy(4-phenylbutyl)phosphoryl]oxyhexanoyl]pyrrolidine-2-carboxylic acid
• 英文别名: Ceranapril; CERONAPRIL; SQ-29,852; Ceronaprilum

物化性质

• 密度: 1.265g/cm3
• 沸点: 682.8ºC at 760 mmHg
• 分子式: C₂₁H₃₃N₂O₆P
• 分子量: 440.47000
• 闪点: 366.7ºC
• 精确质量: 440.20800
• PSA: 139.97000
• LogP: 3.42270
• 蒸汽压: 1.4E-19mmHg at 25°C
• 折射率: 1.559

生物活性

• 描述: Ceronapril(SQ 29852)是一种有效的口服活性血管紧张素转换酶(ACE)抑制剂,IC50为36 nM[1]。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 代谢酶/蛋白酶 >> 血管紧张素转换酶(ACE)
• 靶点:

  IC50: 36 nM (ACE)[1]

• 体内研究: 塞罗那普利(SQ 29852)在雄性 标准差大鼠中抑制 王牌静脉注射和口服的 第50版分别为 0.063μM/kg和 0.53μ塞罗那普利(100 mg/kg；口服；单剂量或每日两次,持续3天)阻断大鼠外周部位的 王牌[2]动物模型：雄性Sprague-Dawley大鼠[2]剂量：100 mg/kg给药：PO,每天两次,连续3天或每天一次。单次给药后迅速(3小时)抑制血浆、肾脏和肺中的ACE。未抑制血脑屏障内大脑结构中的ACE,如尾壳核、脉络丛、苍白球、视上核和下丘脑脑室旁核。
• 参考文献:

  [1]. Karanewsky D S, et al. (Phosphinyloxy) acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy (4-phenylbutyl) phosphinyl] oxy]-1-oxohexyl]-L-proline, a novel orally active inhibitor of ACE. Journal of medicinal chemistry, 1988, 31(1): 204-212.

  [2]. Chen BZ, et al. Effect of acute and chronic administration of ceronapril on angiotensin converting enzyme in plasma, kidney, lung, brain regions and cerebrospinal fluid of rats. Neuropharmacology. 1992 Sep;31(9):929-35.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TW3589050 CHEMICAL NAME : L-Proline, 1-(6-amino-2-((hydroxy(4-phenylbutyl)phosphinyl)oxy)- 1-oxohexyl)-, (S)- CAS REGISTRY NUMBER : 111223-26-8 LAST UPDATED : 199612 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C21-H33-N2-O6-P MOLECULAR WEIGHT : 440.53 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 : >5 gm/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - 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: 20,3875,1992 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2500 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold 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: 20,3875,1992 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse 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: 23,379,1992 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 720 mg/kg SEX/DURATION : female 6-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - other developmental abnormalities 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: 22,3401,1994 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 31 gm/kg SEX/DURATION : female 15-45 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) 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: 22,3401,1994