product name Darunavir Ethanolate
Description: Darunavir Ethanolate (DRV) is a nonpeptidic HIV protease inhibitor, approved by FDA in 2006 to treat HIV infection. Darunavir is an OARAC recommended treatment option for treatment-naive and treatment-experienced adults and adolescents. Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemist who discovered the molecule at the University of Illinois at Chicago (now a Professor at Purdue Univeristy).
References: Biol Pharm Bull. 2009 Sep;32(9):1588-93; Expert Opin Pharmacother. 2007 Aug;8(12):1951-64.
593.73
Formula
C27H37N3O7S.C2H5OH
CAS No.
635728-49-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (168.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
TMC-114, UIC 94017
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Biol Pharm Bull. 2009 Sep;32(9):1588-93; Expert Opin Pharmacother. 2007 Aug;8(12):1951-64. |
