中文名 | Tipranavir |
英文名 | Tipranavir |
别名 | 替拉那韦 替拉那韦杂质1 N-[3-[(1R)-1-[(6R)-2-羟基-4-氧代-6-苯乙基-6-丙基-5H-吡喃-3-基]丙基]苯基]-5-(三氟甲基)吡啶-2-磺酰胺 |
英文别名 | 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 |
化学式 | C31H33F3N2O5S |
分子量 | 602.66 |
密度 | 1.313±0.06 g/cm3(Predicted) |
熔点 | 86-890C |
沸点 | 712.3±70.0 °C(Predicted) |
比旋光度 | D +20° (ethanol) |
溶解度 | 甲醇 (微溶) |
酸度系数 | 4.50±1.00(Predicted) |
存储条件 | -20°C Freezer |
外观 | 固体 |
颜色 | White to Pale Yellow |
体外研究 | 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 (HIV 11MIX ), which include HIV B and HIV C , is selected against Tipranavir, HIV 11MIX rapidly (by 10 passages [HIV 11MIX P10 ]) acquires high-level Tipranavir (PNU-140690) resistance and replicates at high concentrations of Tipranavir (PNU-140690). cHIV B I54V and cHIV B I54V/V82T are significantly resistant to Tipranavir (PNU-140690), with IC 50 s of 2.9 and 3.2 μM, respectively, which are 11- and 12-fold increases in comparison to the IC 50 against cHIV B , respectively. |
体内研究 | 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 [ 14 C]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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.659 ml | 8.297 ml | 16.593 ml |
5 mM | 0.332 ml | 1.659 ml | 3.319 ml |
10 mM | 0.166 ml | 0.83 ml | 1.659 ml |
5 mM | 0.033 ml | 0.166 ml | 0.332 ml |
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