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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Once-daily dolutegravir versus darunavir plus ritonavir for treatment-naive adults with HIV-1 infection (FLAMINGO): 96 week results from a randomised, open-label, phase 3b study.
Molina JM, et al. Lancet HIV. 2015 Apr;2(4):e127-36. PMID: 26424673.
Darunavir: A Review in Pediatric HIV-1 Infection.
Keating GM Paediatr Drugs. 2015 Oct;17(5):411-21. PMID: 26323490.
|Related HIV Protease Products|
BMS-626529 is a potent HIV-1 attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells.
Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy.
Atazanavir is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.
Raltegravir potassium (MK0518 potassium) is a potent integrase (IN) inhibitor, used to treat HIV infection.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.