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Tipranavir

Cat. No. M21645
Tipranavir Structure
Synonym:

PNU-140690

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Biological Activity

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 also inhibits SARS-CoV-2 3CLpro activity. In Tipranavir/ritonavir-cotreated mice, the Tipranavir (PNU-140690) abundance in the liver, spleen, and eyes is significantly higher than that in mice treated with Tipranavir alone.

Chemical Information
Molecular Weight 602.66
Formula C31H33F3N2O5S
CAS Number 174484-41-4
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Tipranavir

[2] No authors listed. Tipranavir

[3] Jennifer S Orman, et al. Drugs. Tipranavir: a review of its use in the management of HIV infection

[4] Zelalem Temesgen, et al. Drugs Today (Barc). Tipranavir

[5] Greg L Plosker, et al. Drugs. Tipranavir

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Keywords: Tipranavir, PNU-140690 supplier, HIV Protease, inhibitors, activators

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