Catalog No.S1620 Synonyms: TMC-114, UIC 94017
Molecular Weight(MW): 593.73
Darunavir Ethanolate (DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
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HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. *P < 0.05, **P < 0.01, ***P < 0.001, 1-way ANOVA with Dunnett’s post-test.
Drug Metab Dispos, 2016, 44(3):398-408.. Darunavir Ethanolate purchased from Selleck.
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Choose Selective HIV Protease Inhibitors
|Description||Darunavir Ethanolate (DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.|
Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM.  Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM. 
|In vitro||DMSO||100 mg/mL (168.42 mM)|
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|Synonyms||TMC-114, UIC 94017|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03094507||Completed||Drug: Tivicay|Drug: Rezolsta||HIV||St Stephens Aids Trust|ViiV Healthcare||April 19 2017||Phase 1|
|NCT03101644||Completed||Drug: Darunavir||Human Immunodeficiency Virus I Infection||Université Catholique de Louvain|Cliniques universitaires Saint-Luc- Université Catholique de Louvain||March 23 2017||Phase 4|
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