产品说明书

Tipranavir

Print
Chemical Structure| 174484-41-4 同义名 : PNU-140690
CAS号 : 174484-41-4
货号 : A278506
分子式 : C31H33F3N2O5S
纯度 : 99%+
分子量 : 602.664
MDL号 : MFCD00949098
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 190 mg/mL(315.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(74.67 mM)，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 Tipranavir (PNU-140690) acts to inhibit the enzymatic function and dimerization of the HIV-1 protease, displaying strong efficacy against HIV-1 strains resistant to multiple protease inhibitors, with IC50 values ranging from 66 to 410 nM[1][2]. Tipranavir is effective in inhibiting the activity of 3CLpro in SARS-CoV-2[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00197145 Infection, Human Immunodeficie... 展开 >>ncy Virus I 收起 << Phase 3 Terminated - -
NCT00708162 HIV Infection Phase 3 Completed - -
NCT00042289 HIV Infections Phase 4 Recruiting September 30, 2019 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.30mL

1.66mL

0.83mL

16.59mL

3.32mL

1.66mL
参考文献

[1]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.

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

[3]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.