145733-36-4

• 常用中文名：他索沙坦
• 常用英文名：Tasosartan
• CAS号：145733-36-4
• 分子式：C₂₃H₂₁N₇O
• 分子量：411.459
• 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
• 发布时间：2018-08-29 19:18:36
• 更新时间：2026-07-01 15:08:41
• Tasosartan 是一种长效的血管紧张素 II (AngII) 受体拮抗剂。

名称

• 中文名: 他索沙坦
• 英文名: 2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
• 中文别名: 塔索萨坦; 8-((2'-(1H-四唑-5-基)-[1,1'-联苯] -4-基)甲基)-2,4-二甲基-5,6-二氢吡啶并[2,3-D ]嘧啶-7(8H) - 酮; Tasostan 10mg试剂; Tasostan试剂; 他沙索坦; 他索沙坦,10 MM DMSO 溶液; 2,4-二甲基-8-[[4-[2-(2H-四唑-5-基)苯基]苯基]甲基]-5,6-二氢吡啶并[6,5-D]嘧啶-7-酮
• 英文别名: 2,4-Dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[6,5-d]pyrimidin-7-one; AC1Q6LAA; 2,4-dimethyl-8-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one; Tasostan, 10 mM in DMSO; ANA-756; 2,4-Dimethyl-8-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one; Tasosta; 2,4-Dimethyl-8-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one; 8-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6h)-one; 8-[2'-(1H-tetrazol-5-yl)-biphenyl-4-yl-methyl]-2,4-dimethyl-5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one; 5,8-Dihydro-2,4-dimethyl-8-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6H)-one; DB01349; S1539_Selleck; Verdia; Pyrido[2,3-d]pyrimidin-7(6H)-one, 5,8-dihydro-2,4-dimethyl-8-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]; 8-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,6-dihydropyrido[2,3-d]pyrimidin-7(8H)-one; TASOSTAN; 2,4-dimethyl-5,6,8-trihydro-8-[[2'-(1H-tetrazol-5-yl)[1,1-biphenyl]-4-yl]methyl]-7H-pyrido[2,3-d]pyrimidin-7-one; 2,4-dimethyl-8-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one; Tasosartan (USAN/INN); AC1L1U5X; WAY-ANA-756; VERDIA; S1539_SELLECK; ANA-756; AC1Q6LAA; TASOSTAN (USAN/INN); DB01349; TASOSTAN; AC1L1U5X; WAY-ANA-756; Tasostan (USAN/INN); Inhibitor,Angiotensin Rector,inhibit,Tasostan; tasosartan

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 759.4±70.0 °C at 760 mmHg
• 分子式: C₂₃H₂₁N₇O
• 分子量: 411.459
• 闪点: 413.1±35.7 °C
• 精确质量: 411.180756
• PSA: 100.55000
• LogP: 2.62
• 蒸汽压: 0.0±2.6 mmHg at 25°C
• 折射率: 1.665
• 储存条件: 2-8℃

生物活性

• 描述: Tasosartan 是一种长效的血管紧张素 II (AngII) 受体拮抗剂。
• 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
• 靶点:

  Angiotensin II (AngII) receptor[1]

• 体外研究: Tasosartan是一种口服活性非肽AngII拮抗剂,在体外具有特异性和选择性AT1受体拮抗活性。在结合缓冲液中不存在蛋白质时抑制125I-AngII与大鼠肾上腺膜特异性结合的IC 50为1.2±0.6nM [1]。
• 体内研究: 以1.0和3.0mg/kg(iv)的剂量给予Tasosartan显着(p <0.05)减弱了大鼠对血管紧张素-II的升压反应[2]。
• 动物实验: 大鼠[2]对四组大鼠（每组n = 3-5，体重343±8g）施用血管紧张素-II的压力反应。在引入载体或分级剂量的Tasosartan（0.3,1.0或3.0mg / kg，iv）后，对每只大鼠进行四次单独的血管紧张素-II注射[2]。
• 参考文献:

  [1]. Maillard MP, et al. Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.

  [2]. Elokdah HM, et al. Novel human metabolites of the angiotensin-II antagonist Tasosartan and their pharmacological effects. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71.

合成路线

149049-80-9 ~39% 145733-36-4

文献：American Home Products Corporation Patent: US5149699 A1, 1992 ; US 5149699 A

153042-17-2 ~73% 145733-36-4

文献：Ellingboe, John W.; Antane, Madelene; Nguyen, Thomas T.; Collini, Michael D.; Antane, Schuyler; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 4 p. 542 - 550

1501-06-0 ~% 145733-36-4

文献：Journal of Medicinal Chemistry, , vol. 37, # 4 p. 542 - 550

22814-39-7 ~% 145733-36-4

文献：Journal of Medicinal Chemistry, , vol. 37, # 4 p. 542 - 550

22814-29-5 ~% 145733-36-4

文献：Journal of Medicinal Chemistry, , vol. 37, # 4 p. 542 - 550

145733-62-6 ~% 145733-36-4

文献：Journal of Medicinal Chemistry, , vol. 37, # 4 p. 542 - 550

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