Tipranavir-d4

• 常用名: Tipranavir-d4
• 英文名: Tipranavir-d4
• CAS号: 1217819-15-2
• 分子量: 602.664
• 密度: 1.3±0.1 g/cm3
• 沸点: 712.3±70.0 °C at 760 mmHg
• 分子式: C₃₁H₃₃F₃N₂O₅S
• 熔点: N/A
• 闪点: 384.6±35.7 °C

Tipranavir-d4用途

Tipranavir-d4(PNU-140690-d4)是氘标记的Tipranavir。Tipranavir(PNU-140690)抑制HIV-1蛋白酶的酶活性和二聚化,对IC50s为66-410 nM的耐多蛋白酶抑制剂(PI)的HIV-1分离株发挥有效活性[1][2]。蒂普拉那韦抑制SARS-CoV-2 3CLpro活性[3]。

Tipranavir-d4名称

• 中文名: 替拉那韦-D4
• 英文名: Tipranavir-d4

Tipranavir-d4生物活性

• 描述: Tipranavir-d4(PNU-140690-d4)是氘标记的Tipranavir。Tipranavir(PNU-140690)抑制HIV-1蛋白酶的酶活性和二聚化,对IC50s为66-410 nM的耐多蛋白酶抑制剂(PI)的HIV-1分离株发挥有效活性[1][2]。蒂普拉那韦抑制SARS-CoV-2 3CLpro活性[3]。
• 相关类别:
  信号通路 >> 抗感染 >> HIV
  研究领域 >> 感染
  信号通路 >> 抗感染 >> SARS冠状病毒
  信号通路 >> 代谢酶/蛋白酶 >> HIV蛋白酶
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96.

  [3]. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 May;38(5):871-8.

  [4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

Tipranavir-d4物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 712.3±70.0 °C at 760 mmHg
• 分子式: C₃₁H₃₃F₃N₂O₅S
• 分子量: 602.664
• 闪点: 384.6±35.7 °C
• 精确质量: 602.206238
• LogP: 7.20
• 蒸汽压: 0.0±2.4 mmHg at 25°C
• 折射率: 1.579
• 储存条件: -20°C，干燥，密封

Tipranavir-d4安全信息

• 危害码 (欧洲): Xi

Tipranavir-d4英文别名

• N-(3-{(1R)-1-[(6R)-4-hydroxy-2-oxo-6-(2-phényléthyl)-6-propyl-5,6-dihydro-2H-pyran-3-yl]propyl}phényl)-5-(trifluorométhyl)pyridine-2-sulfonamide
• 2-Pyridinesulfonamide, N-(3-((1R)-1-((6R)-5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl)propyl)phenyl)-5-(trifluoromethyl)-
• N-(3-{(1R)-1-[(6R)-4-Hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-5,6-dihydro-2H-pyran-3-yl]propyl}phenyl)-5-(trifluoromethyl)-2-pyridinesulfonamide
• ZZT404XD09
• 2-Pyridinesulfonamide, N-[3-[(1R)-1-[(6R)-5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-
• N-[3-[(1R)-1-[(6R)-5,6-Dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide
• Tipranavir
• MFCD00949098
• N-(3-{(1R)-1-[(6R)-4-Hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-5,6-dihydro-2H-pyran-3-yl]propyl}phenyl)-5-(trifluormethyl)pyridin-2-sulfonamid
• N-(3-{(1R)-1-[(6R)-4-Hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-5,6-dihydro-2H-pyran-3-yl]propyl}phenyl)-5-(trifluoromethyl)pyridine-2-sulfonamide
• N-(3-{(1R)-1-[(6R)-4-HYDROXY-2-OXO-6-PHENETHYL-6-PROPYL-5,6-DIHYDRO-2H-PYRAN-3-YL]PROPYL}PHENYL)-5-(TRIFLUOROMETHYL)-2-PYRIDINESULFONAMIDE
• PNU 140690E
• [R-(R*,R*)]-N-[3-[1-[5,6-Dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide
• aptivus