54504-70-0

• 常用中文名：益多酯
• 常用英文名：etofylline clofibrate
• CAS号：54504-70-0
• 分子式：C₁₉H₂₁ClN₄O₅
• 分子量：420.847
• 相关类别： 原料药 循环系统用药 调节血脂药
• 发布时间：2018-04-06 08:00:00
• 更新时间：2024-01-08 11:21:28
• Etofylline clofibrate 具有降脂和抗血栓形成作用。Etofylline clofibrate 具有与内膜 PGI2 激动的相互作用。

名称

• 中文名: 益多酯
• 英文名: 2-(1,3-dimethyl-2,6-dioxopurin-7-yl)ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
• 中文别名: 乙羟茶碱安妥明酯
• 英文别名: 2-(4-Chlorophenoxy)-2-methylpropanoic Acid 2-(1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-7H-purin-7-yl)ethyl Ester; etofylline clofibrate; etofyllinclofibrate; Theofibrate; Propanoic acid, 2-(4-chlorophenoxy)-2-methyl-, 2-(1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-7H-purin-7-yl)ethyl ester; 2-(p-Chlorophenoxy)-2-methylpropionic acid 2-(7-theophyllinyl)ethyl ester; 2-(p-Chlorophenoxy)-2-methylpropionic Acid Ester with 7-(2-Hydroxyethyl)theophylline; Propionic acid, 2-(p-chlorophenoxy)-2-methyl-, 2-(7-theophyllinyl)ethyl ester; Etofyllinclofibrat; 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)ethyl 2-(4-chlorophenoxy)-2-methylpropanoate; Duolip; 2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)ethyl 2-[(4-chlorophenyl)oxy]-2-methylpropanoate

物化性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 615.8±65.0 °C at 760 mmHg
• 熔点: 133-135°
• 分子式: C₁₉H₂₁ClN₄O₅
• 分子量: 420.847
• 闪点: 326.2±34.3 °C
• 精确质量: 420.120056
• PSA: 97.35000
• LogP: 2.75
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.618

生物活性

• 描述: Etofylline clofibrate 具有降脂和抗血栓形成作用。Etofylline clofibrate 具有与内膜 PGI2 激动的相互作用。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 其他 >> 其他
• 体内研究: 依托普林氯贝特酯(P.O；12 mg/kg)具有单一剂量的中度效应(解聚时间的12%减少),分别在5次和7次连续应用后分别最大降低31和43% [1 ]。
• 参考文献:

  [1]. Metz G, et al. Effect of etofylline clofibrate on experimental thrombus formation and prostacyclin activation. Arzneimittelforschung. 1986 Sep;36(9):1363-5.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UE9516500 CHEMICAL NAME : Propionic acid, 2-(4-chlorophenoxy)-2-methyl-, 2-(1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo- 7H-purin-7-yl) ethyl ester CAS REGISTRY NUMBER : 54504-70-0 LAST UPDATED : 199612 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C19-H21-Cl-N4-O5 MOLECULAR WEIGHT : 420.89 WISWESSER LINE NOTATION : T56 BM DN FNVNVTJ D2OVX1&1&OR DG& F1 H1 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 : 17000 mg/kg TOXIC EFFECTS : Liver - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2830 mg/kg TOXIC EFFECTS : Liver - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,1173,1977 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 27300 mg/kg/26W-I TOXIC EFFECTS : Behavioral - fluid intake Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - pig DOSE/DURATION : 146 gm/kg/26W-I TOXIC EFFECTS : Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 8250 mg/kg SEX/DURATION : female 5-15 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 4200 mg/kg SEX/DURATION : female 14 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 21 gm/kg SEX/DURATION : male 70 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,2023,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 7500 mg/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,1173,1977 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 117 mg/kg SEX/DURATION : female 7-16 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - other developmental abnormalities REFERENCE : PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 64,286,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 5855 mg/kg SEX/DURATION : female 7-16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - urogenital system REFERENCE : PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 64,286,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 7800 mg/kg SEX/DURATION : female 6-18 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 : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,1173,1977

合成路线

5542-60-9 519-37-9 ~82% 54504-70-0

文献：Metz; Specker Arzneimittel-Forschung/Drug Research, 1980 , vol. 30, # 116 p. 2014 - 2019

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