1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV Protease
    HIV
    SARS-CoV
  3. Tipranavir

Tipranavir (Synonyms: PNU-140690)

Cat. No.: HY-15148 Purity: 99.77%
Handling Instructions

Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CLpro activity.

For research use only. We do not sell to patients.

Tipranavir Chemical Structure

Tipranavir Chemical Structure

CAS No. : 174484-41-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 636 In-stock
Estimated Time of Arrival: December 31
1 mg USD 154 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

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Description

Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].

IC50 & Target

IC50: 66-410 nM (HIV-1 isolates)[1]

In Vitro

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 (HIV11MIX), which include HIVB and HIVC, is selected against Tipranavir, HIV11MIX rapidly (by 10 passages [HIV11MIXP10]) acquires high-level Tipranavir (PNU-140690) resistance and replicates at high concentrations of Tipranavir (PNU-140690). cHIVBI54V and cHIVBI54V/V82T are significantly resistant to Tipranavir (PNU-140690), with IC50s of 2.9 and 3.2 μM, respectively, which are 11- and 12-fold increases in comparison to the IC50 against cHIVB, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 [14C]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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

602.66

Formula

C₃₁H₃₃F₃N₂O₅S

CAS No.
SMILES

O=C1C([[email protected]](CC)C2=CC=CC(NS(C3=CC=C(C(F)(F)F)C=N3)(=O)=O)=C2)=C(O)C[[email protected]](CCC4=CC=CC=C4)(CCC)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (331.86 mM; Need ultrasonic)

Ethanol : ≥ 50 mg/mL (82.97 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (8.30 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (8.30 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

  • 4.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

  • 5.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

  • 6.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Mice[2]
All mice (2-4 months old) are maintained under a standard 12-h dark and 12-h light cycle with water and chow provided ad libitum. For metabolomic analysis, Tipranavir (PNU-140690) (40 mg/kg) is administered via ball-tipped gavage needles, and the mice are housed in separate metabolic cages for 18 h. Urine and feces samples are collected and stored at −20°C for further analysis. For tissue distribution and inhibition studies, three groups of mice are used and are orally treated with Tipranavir (100 mg/kg), RTV (40 mg/kg), and Tipranavir (PNU-140690) (100 mg/kg Tipranavir and 40 mg/kg RTV), respectively. Tissues including the liver, brain, lung, kidney, spleen, and eyes are collected 30 min after treatment and stored at −20°C for further analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

TipranavirPNU-140690PNU140690PNU 140690HIV ProteaseHIVSARS-CoVHuman immunodeficiency virusSARS coronavirusInhibitorinhibitorinhibit

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Tipranavir
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