替拉那韦
中文名称 | 替拉那韦 |
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中文同义词 | 替拉那韦;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;替拉那韦杂质1;N-(3-((R)-1-((R)-4-羟基-2-氧代-6-苯乙基-6-丙基-5,6-二氢-2H-吡喃-3-基)丙基)苯基)-5-(三氟甲基)吡啶-2-磺酰胺 |
英文名称 | Tipranavir |
英文同义词 | PNU-140690;Aptivus;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;N-[3-[(1R)-1-[(6R)-2-Hydroxy-4-oxo-6-phenethyl-6-propyl-5H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)pyridine-2-sulfonamide;Tipranavir;Tipranavir(PNU-140690,Aptivus);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)-;Tipranavir(TPV) |
CAS号 | 174484-41-4 |
分子式 | C31H33F3N2O5S |
分子量 | 602.66 |
EINECS号 | |
相关类别 | 医药中间体;抗病毒类;All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Antiviral Agents |
Mol文件 | 174484-41-4.mol |
结构式 |
替拉那韦 性质
熔点 | 86-890C |
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比旋光度 | D +20° (ethanol) |
沸点 | 712.3±70.0 °C(Predicted) |
密度 | 1.313±0.06 g/cm3(Predicted) |
储存条件 | -20°C Freezer |
溶解度 | 少许溶于甲醇 |
形态 | 固体 |
酸度系数(pKa) | 4.50±1.00(Predicted) |
颜色 | 白色至浅黄色 |
BCS Class | 2 |
IC50: 66-410 nM (HIV-1 isolates)
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-15148 | 替拉那韦 Tipranavir | 174484-41-4 | 1mg | 950元 |
2024/01/25 | HY-15148 | 替拉那韦 Tipranavir | 174484-41-4 | 5mg | 3300元 |