PNU-140690 MedChemExpress (MCE)

Product Name	Tipranavir
Synonyms	Aptivus PNU-140690 Tipranavir Tipranavir(TPV) TIPRANAVIR (PNU-140690) N-[3-[(1R)-1-[(6R)-2-Hydroxy-4-oxo-6-phenethyl-6-propyl-5H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)pyridine-2-sulfonamide Synonyms Aptivus PNU-140690 Tipranavir Tipranavir(TPV) TIPRANAVIR (PNU-140690) N-[3-[(1R)-1-[(6R)-2-Hydroxy-4-oxo-6-phenethyl-6-propyl-5H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)pyridine-2-sulfonamide N-[3-[(1R)-1-[(2R)-4-HYDROXY-6-OXO-2-(2-PHENYLETHYL)-2-PROPYL-3H-PYRAN-5-YL]PROPYL]PHENYL]-5-(TRIFLUOROMETHYL)PYRIDINE-2-SULFONAMIDE 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
CAS	174484-41-4
EINECS
Chemical Formula	C31H33F3N2O5S
Molecular Weight	602.66
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	Tipranavir Tipranavir MedChemExpress (MCE) HY-15148 174484-41-4 PNU-140690 98.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Tipranavir Tipranavir MedChemExpress (MCE) HY-15148 174484-41-4 PNU-140690 98.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CLpro activity. Tipranavir (PNU-140690) inhibits the enzymatic activity of HIV-1 protease, blocks the dimerization of protease subunits, and exerts potent activity against a wide spectrum of wild-type and multi-PI-resistant HIV-1 variants. When a mixture of 11 multi-PI-resistant (but TPV-sensitive) clinical isolates (HIV11MIX), which include HIVB and HIVC, is selected against Tipranavir, HIV11MIX rapidly (by 10 passages [HIV11MIXP10]) acquires high-level Tipranavir (PNU-140690) resistance and replicates at high concentrations of Tipranavir (PNU-140690). cHIVBI54V and cHIVBI54V/V82T are significantly resistant to Tipranavir (PNU-140690), with IC50s of 2.9 and 3.2 μM, respectively, which are 11- and 12-fold increases in comparison to the IC50 against cHIVB, respectively[1]. Tipranavir (PNU-140690) is administered orally twice daily and must be given in combination with low-dose ritonavir (RTV) to boost Tipranavir bioavailability. In Tipranavir/r-cotreated mice, the Tipranavir (PNU-140690) abundance in the liver, spleen, and eyes is significantly higher than that in mice treated with Tipranavir alone. Tipranavir (PNU-140690) metabolites accounts for 31 and 38% in the serum and liver in the Tipranavir-alone group. In Tipranavir (PNU-140690) and Tipranavir (TPV/r)-cotreated mice, only 1 and 2% of metabolites are detected in the serum and liver. Sprague-Dawley rats are administered a single dose of [14C]Tipranavir (PNU-140690) with coadministration of RTV. The most abundant metabolite in feces is an oxidation metabolite. In urine, no single metabolite is found to be significantly present[2]. Mice[2] All mice (2-4 months old) are maintained under a standard 12-h dark and 12-h light cycle with water and chow provided ad libitum. For metabolomic analysis, Tipranavir (PNU-140690) (40 mg/kg) is administered via ball-tipped gavage needles, and the mice are housed in separate metabolic cages for 18 h. Urine and feces samples are collected and stored at −20°C for further analysis. For tissue distribution and inhibition studies, three groups of mice are used and are orally treated with Tipranavir (100 mg/kg), RTV (40 mg/kg), and Tipranavir (PNU-140690) (100 mg/kg Tipranavir and 40 mg/kg RTV), respectively. Tissues including the liver, brain, lung, kidney, spleen, and eyes are collected 30 min after treatment and stored at −20°C for further analysis. HIV-1 \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]
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Last Update	2025-05-21 16:50:25

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