Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
Purity: ≥98%
Tipranavir (PNU140690; PNU-140690; trade name: Aptivus) is a marketed anti-HIV drug acting as a nonpeptidic multi-protease inhibitor (IC50s = 66-410 nM). Tipranavir is able to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with some drug resistance.
Targets |
|
|
---|---|---|
ln Vitro |
Tipranavir (PNU-140690) exhibits strong action against a broad range of wild-type and multi-PI-resistant HIV-1 variants, inhibits the enzymatic activity of HIV-1 protease, and prevents the dimerization of protease subunits. HIV11MIX, a mixture of 11 multi-PI-resistant (but TPV-sensitive) clinical isolates (including HIVB and HIVC), quickly develops high-level Tipranavir (PNU-140690) resistance and replicates at high concentrations of Tipranavir (PNU-140690) after being selected against Tipranavir (by 10 passages [HIV11MIXP10]). With IC50s of 2.9 and 3.2 μM, respectively, which represent 11- and 12-fold increases in comparison to the IC50 against cHIVB, cHIVBI54V and cHIVBI54V/V82T are considerably resistant to Tipranavir (PNU-140690)[1].
|
|
ln Vivo |
To increase the bioavailability of dipranavir (PNU-140690), it is necessary to combine it with low-dose ritonavir (RTV) when given orally twice a day. The abundance of Tipranavir (PNU-140690) in the liver, spleen, and eyes is considerably higher in Tipranavir/r-cotreated mice than in Tipranavir-treated animals. In the Tipranavir-alone group, 31 and 38% of the serum and liver, respectively, are made up of metabolites of tipranavir (PNU-140690). In the serum and liver of mice cotreated with tipranavir (PNU-140690) and tipranavir (TPV/r), respectively, only 1 and 2% of metabolites are found. One dose of [14C]Tipranavir (PNU-140690) is given to Sprague-Dawley rats in conjunction with RTV. Feces include a lot of oxidation-related metabolites. There isn't a single metabolite that is discovered to be substantially present in urine[2].
|
|
Animal Protocol |
|
|
References |
[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.
[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. [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 |
Molecular Formula |
C31H33N2O5F3S
|
---|---|
Molecular Weight |
602.66432
|
CAS # |
174484-41-4
|
SMILES |
O=C1C([C@H](CC)C2=CC=CC(NS(C3=CC=C(C(F)(F)F)C=N3)(=O)=O)=C2)=C(O)C[C@](CCC4=CC=CC=C4)(CCC)O1
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~200 mg/mL (~331.86 mM)
Ethanol :≥ 50 mg/mL (~82.97 mM) |
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6593 mL | 8.2966 mL | 16.5931 mL | |
5 mM | 0.3319 mL | 1.6593 mL | 3.3186 mL | |
10 mM | 0.1659 mL | 0.8297 mL | 1.6593 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.