| Description | Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity. |
| In vitro | Tipranavir (PNU-140690) 抑制 HIV-1 蛋白酶的酶活性，阻断蛋白酶亚单位的二聚化，并对广泛的野生型和多重PI抗性HIV-1变种展现出强大的活性。[1] |
| In vivo | Tipranavir（5 mg/kg；小鼠模型）：其CLtot为0.17 ± 0.10 L/h/kg，Vss为0.51 ± 0.14 L/kg，t1/2为5.4 ± 0.3h。[4] 在大鼠模型下，通过口服给药（10 mg/kg）得出Tipranavir的生物利用度（F）与5 mg/kg剂量相比为30%。[4] |
| Target activity | HIV-1 (isolates):66-410 nM, HIV-1 (isolates):8 pM(Ki ) |
| Synonyms | PNU-140690 |
| molecular weight | 602.66 |
| Molecular formula | C31H33F3N2O5S |
| CAS | 174484-41-4 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 45.0 mg/mL (74.7 mM) DMSO: 180.0 mg/mL (298.7 mM ), Sonication is recommended. |
| References | 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-J Virol. 2012 ; 86(24):13384-13396. 2. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 ; 38(5):871-878. 3. Sun Q, 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 ; 6(1):212. 4. Turner SR, et al. Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. J Med Chem. 1998 ; 41(18):3467-3476. |