247257-48-3

• 常用中文名：非马沙坦
• 常用英文名：Fimasartan
• CAS号：247257-48-3
• 分子式：C₂₇H₃₁N₇OS
• 分子量：501.646
• 相关类别： 原料药 循环系统用药 抗高血压病药
• 发布时间：2018-03-19 08:00:00
• 更新时间：2026-06-30 18:28:27
• Fimasartan(BR-A-657)是血管紧张素受体AT1非肽类拮抗剂,用于治疗高血压和心力衰竭。

名称

• 中文名: 非马沙坦
• 英文名: 2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide
• 中文别名: 2-丁基-5-二甲基氨基硫代甲酰甲基-6-甲基-3-[[2'-(1H-四唑-5-基)联苯-4-基]甲基]嘧啶-4(3H)-酮; 非马沙坦游离碱; 2-丁基-1,6-二氢-N,N,4-三甲基-6-氧代-1-[[2'-( 2H-四唑-5-基)[1,1'-联苯]-4-基]甲基]-5-嘧啶乙硫酰胺; 2-(1-((2'-(1H-四氮唑-5-基)-[1,1'-联苯]-4-基)甲基)-2-丁基-4-甲基-6-氧代-1,6-二氢嘧啶-5-基)-N,N-二甲基硫代乙酰胺; 非马沙坦BASE; 飞马沙坦杂质H; 2-(2-丁基-4-甲基-6-羰基-1-((2'-(1-三苯甲基-1氢-四唑-5-基)-[1,1'-联苯]-4-基)甲基)-1,6-二氢嘧啶-5-基)-N,N-二甲基乙酰胺; 飞马沙坦杂质F; 非马沙坦,10 MM DMSO 溶液; 2-(1-((2'-(2H-四唑-5-基)-[1,1'-联苯]-4-基)甲基)-2-叔丁基-4-甲基-6-氧代 6-二氢嘧啶-5-基)-N,N-二甲基乙硫代酰胺; 非马沙坦杂质F; 2-(2-丁基-4-甲基-6-((2'-(1-三苯甲基-1氢-四唑-5-基)-[1,1'-联苯]-4-基)甲氧基)嘧啶-5-基)-N,N-二甲基乙酰胺; 2-N-丁基-5-二甲胺基硫代羰基甲基-6-甲基-3[2'-(1H-四唑-5-基)联苯-4-基]甲基嘧啶-4(3H)-酮; 非马沙坦杂质H; 2-(2-丁基-4-甲基-6-((2'-(1-三苯甲基-1氢; 非马沙坦FIMASTAN
• 英文别名: 5-PyriMidineethanethioaMide,2-butyl-1,6-dihydro-N,N,4-triMethyl-6-oxo-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]; Fimastan; 2-(2-butyl-4-Methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)Methyl)-1,6-dihydropyriMidin-5-yl)-N,N-diMethylethanethioaMide; Kanb; KANB; BR-A-657; Fimastan(BR-A-657); 2-(2-Butyl-4-methyl-6-oxo-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl] methyl}-1,6-dihydro-5-pyrimidinyl)-N,N-dimethylethanethioamide (Fimastan); Non-mastan; Fimastan, 10 mM in DMSO; Fimastan Impurity H; UNII-P58222188P; br-a-657k; FiMastan //BP; 2-(1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-N,N-dimethylethanethioamide; 2-(2-butyl-4-Methyl-6-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)Methoxy)pyriMidin-5-yl)-N,N-diMethylacetaMide-yl)-N,N-diMethylacetaMide; 2-(2-Butyl-4-methyl-6-oxo-1-{[2'-(2H-tetrazol-5-yl)-4-biphenylyl]methyl}-1,6-dihydro-5-pyrimidinyl)-N,N-dimethylethanethioamide; 2-(1-((2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-N,N-dimethylethanethioamide; Fimastan D4; BR-A-657; 2-(2-butyl-4-methyl-6-((2'-(1-trityl-1H-tetrazol-5-yl)-[ 1,1'-biphenyl]-4-yl)methoxy)pyrimidin-5-yl)-N,N- dimethylacetamide; 2-Butyl-5-dimethylaminothiocbonylmethyl-6-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one; Unii-p58222188p; 5-Pyrimidineethanethioamide, 2-butyl-1,6-dihydro-N,N,4-trimethyl-6-oxo-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]; 2-Butyl-5-dimethylaminothiocbonylmethyl-6-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one //BP; 2-(2-Butyl-4-methyl-6-oxo-1-{[2'-(1H-tetrazol-5-yl)- 4-biphenylyl]methyl}-1,6-dihydro-5-pyrimidinyl)- N,N-dimethylethanethioamide; 2-(1-((2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrim

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 693.0±65.0 °C at 760 mmHg
• 分子式: C₂₇H₃₁N₇OS
• 分子量: 501.646
• 闪点: 372.9±34.3 °C
• 精确质量: 501.231079
• PSA: 124.68000
• LogP: 4.53
• 外观性状: 粉末
• 蒸汽压: 0.0±2.2 mmHg at 25°C
• 折射率: 1.658
• 储存条件: -20℃

生物活性

• 描述: Fimasartan(BR-A-657)是血管紧张素受体AT1非肽类拮抗剂,用于治疗高血压和心力衰竭。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管紧张素受体
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Ryu S, et al. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36(3):467-74.

  [2]. Chi YH, et al. Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist. Biol Pharm Bull. 2013;36(7):1208-15.

  [3]. Lee HW, et al. Effect of age on the pharmacokinetics of fimasartan (BR-A-657). Expert Opin Drug Metab Toxicol. 2011 Nov;7(11):1337-44.

  [4]. Shin KH, et al. The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers. J Cardiovasc Pharmacol. 2011 Nov;58(5):492-9.

合成路线

503155-65-5 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654

503155-66-6 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654

1361024-33-0 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654

503155-67-7 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654

1361024-52-3 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654

110-59-8 ~% 247257-48-3

文献：Kim, Tae Woo; Yoo, Byoung Wook; Lee, Joon Kwang; Kim, Ji Han; Lee, Kyung-Tae; Chi, Yong Ha; Lee, Jae Yeol Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1649 - 1654