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
Tipranavir
CAS: 174484-41-4
Molecular Formula: C31H33F3N2O5S
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 - Names and Identifiers
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 - Physico-chemical Properties
| Molecular Formula | C31H33F3N2O5S |
| Molar Mass | 602.66 |
| Density | 1.313±0.06 g/cm3(Predicted) |
| Melting Point | 86-890C |
| Boling Point | 712.3±70.0 °C(Predicted) |
| Specific Rotation(α) | D +20° (ethanol) |
| Solubility | Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Pale Yellow |
| pKa | 4.50±1.00(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | 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. |
| In vivo study | 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. |
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 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
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View History
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
2-苯基-4-噻唑烷-4-羧酸
2-(6-氯吡啶吡啶-2-基)丙-2-醇
(S)-(4-甲基-1-吗啉-1-氧戊烷-2-基)氨基甲酸叔丁酯
(-)二异松蒎基硼烷
ASCORBIC ACID 2-PHOSPHATE MAGNESIUM ESTER
二氯双[3-(二异丙基膦基)丙基氨]钌(II)
2-乙基-5,7-二甲基-3H-咪唑并[4,5-Β]吡啶
3-氨基-6-氯吡啶-2-甲酰胺
2-氨基-5,5-二甲基-4,7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸叔丁酯
2-苯基-4-噻唑烷-4-羧酸
2-(6-氯吡啶吡啶-2-基)丙-2-醇
(S)-(4-甲基-1-吗啉-1-氧戊烷-2-基)氨基甲酸叔丁酯
(-)二异松蒎基硼烷
ASCORBIC ACID 2-PHOSPHATE MAGNESIUM ESTER
二氯双[3-(二异丙基膦基)丙基氨]钌(II)
2-乙基-5,7-二甲基-3H-咪唑并[4,5-Β]吡啶
3-氨基-6-氯吡啶-2-甲酰胺
2-氨基-5,5-二甲基-4,7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸叔丁酯