替拉那韦

抗病毒药生物活性靶点体外研究体内研究替拉那韦试剂级价格

替拉那韦

CAS号:174484-41-4
英文名:Tipranavir
中文名:替拉那韦
CBNumber:CB9501005
分子式:C31H33F3N2O5S
分子量:602.66
MOL File:174484-41-4.mol

替拉那韦化学性质

熔点 :86-890C
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 :Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :4.50±1.00(Predicted)
颜色 :White to Pale Yellow
BCS Class :2

安全信息

毒害物质数据 :174484-41-4(Hazardous Substances Data)

替拉那韦性质、用途与生产工艺

抗病毒药替拉那韦，西药名。常用剂型有胶囊剂等。为抗病毒药。合用利托那韦对具有病毒复制、并已治疗时间很长或感染HIV-1面又耐多种蛋白酶抑制剂的成年患者进行治疗。
生物活性 Tipranavir (PNU-140690) 有效抑制 HIV-1 蛋白酶酶活性和二聚化，对抗多种蛋白酶抑制剂(PI)的HIV-1分离株具有有效的活性，IC50 为 66-410 nM。
靶点

IC50: 66-410 nM (HIV-1 isolates)
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.