103475-41-8

• 常用中文名：替泊沙林
• 常用英文名：Tepoxalin
• CAS号：103475-41-8
• 分子式：C₂₀H₂₀ClN₃O₃
• 分子量：385.844
• 发布时间：2018-03-26 08:00:00
• 更新时间：2024-01-02 14:53:20
• 替泊沙林是COX和5-脂氧合酶(5-LO)的双重抑制剂,具有强大的抗炎活性和良好的胃肠道状况[1]。

名称

• 中文名: 替泊沙林
• 英文名: tepoxalin
• 英文别名: Zubrin; Tepoxalinum [Latin]; 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-methylpropanamide; 1H-Pyrazole-3-propanamide, 5-(4-chlorophenyl)-N-hydroxy-1-(4-methoxyphenyl)-N-methyl-; 5-(4-chlorophenyl)-N-hydroxy-1-(4-methoxyphenyl)-N-methyl-1H-pyrazole-3-propanamide; Tepoxalin; Tepoxalin [USAN:INN]; Tepoxaline; Tepoxalina [Spanish]; Tepoxalina; 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]-N-hydroxy-N-methylpropanamide; 3-[5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-1H-pyrazol-3-yl]-N-hydroxy-N-methylpropanamide; Tepoxaline [French]

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 573.0±60.0 °C at 760 mmHg
• 分子式: C₂₀H₂₀ClN₃O₃
• 分子量: 385.844
• 闪点: 300.3±32.9 °C
• 精确质量: 385.119324
• PSA: 67.59000
• LogP: 3.84
• 蒸汽压: 0.0±1.7 mmHg at 25°C
• 折射率: 1.610

生物活性

• 描述: 替泊沙林是COX和5-脂氧合酶(5-LO)的双重抑制剂,具有强大的抗炎活性和良好的胃肠道状况[1]。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> 免疫及炎症 >> COX
  信号通路 >> 代谢酶/蛋白酶 >> 5脂氧合酶
• 参考文献:

  [1]. Argentieri DC, et al. Tepoxalin: a dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile. J Pharmacol Exp Ther. 1994 Dec;271(3):1399-408.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UQ8002500 CHEMICAL NAME : 1H-Pyrazole-3-propanamide, 5-(4-chlorophenyl)-N-hydroxy-1-(4-methoxyphenyl)-N-me thyl- CAS REGISTRY NUMBER : 103475-41-8 LAST UPDATED : 199712 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C20-H20-Cl-N3-O3 MOLECULAR WEIGHT : 385.88 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1085 mg/kg/31D-I TOXIC EFFECTS : Blood - pigmented or nucleated red blood cells Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in erythrocyte (RBC) count REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 33,38,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 7280 mg/kg/26W-I TOXIC EFFECTS : Liver - changes in liver weight Blood - pigmented or nucleated red blood cells Blood - changes in erythrocyte (RBC) count REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 33,38,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 54600 mg/kg/26W-I TOXIC EFFECTS : Gastrointestinal - alteration in gastric secretion Gastrointestinal - ulceration or bleeding from stomach REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 33,38,1996

合成路线

19501-58-7 142791-64-8 ~71% 103475-41-8 149065-93-0

文献：Journal of Organic Chemistry, , vol. 57, # 24 p. 6662 - 6663

111881-78-8 ~% 103475-41-8

文献：Journal of Organic Chemistry, , vol. 57, # 24 p. 6662 - 6663

142791-63-7 ~% 103475-41-8

文献：Journal of Organic Chemistry, , vol. 57, # 24 p. 6662 - 6663

144192-64-3 ~% 103475-41-8

文献：Journal of Organic Chemistry, , vol. 57, # 24 p. 6662 - 6663

19501-58-7 ~% 103475-41-8

文献：Synthesis, , # 1 p. 18 - 20

114150-42-4 ~% 103475-41-8

文献：Synthesis, , # 1 p. 18 - 20

4229-44-1 114151-49-4 ~% 103475-41-8

文献：Synthesis, , # 1 p. 18 - 20

144192-63-2 ~% 103475-41-8

文献：Journal of Organic Chemistry, , vol. 57, # 24 p. 6662 - 6663

上下游产品

上游产品  6
19501-58-7 111881-78-8 142791-63-7 144192-63-2
114150-42-4 4229-44-1
下游产品  0