DPC-681

DPC-681 (2-20 μM; 3 days) induces CYP3A4 protein expression in primary human hepatocytes in a concentration-dependent manner^[1].
DPC-681 (2-20 μM; 3 days) does not significantly induce measurable CYP3A4 testosterone 6β-hydroxylase activity in primary human hepatocytes^[1].
DPC-681 (2-20 μM; 3 days) induces CYP3A testosterone 6β-hydroxylase activity approximately 3-fold over vehicle control in primary male and female Sprague-Dawley rat hepatocytes^[1].
DPC-681 (0.002-12.5 μM; 10 min) potently inhibits human CYP3A4-mediated testosterone 6β-hydroxylation in pooled human liver microsomes with an IC₅₀ of 0.039 μM^[1].
DPC-681 (0.002-12.5 μM; 10 min) inhibits rat CYP3A-mediated testosterone 6β-hydroxylation in pooled Sprague-Dawley rat liver microsomes with an IC₅₀ of 1.62 μM, which is 40-fold less potent than its inhibition of human CYP3A4^[1].
DPC-681 potently inhibits wild-type HIV-1 protease with a mean K_i value of 0.012 nM^[2].
DPC-681 is highly selective for HIV-1 protease, with less than 50% inhibition of tested cellular proteases at concentrations of ≥13 μM^[2].
DPC-681 (3-7 days) potently inhibits replication of wild-type HIV-1 strains, non-clade B isolates, and HIV-2 in MT-2, MT-4, and PBMC, with a mean IC₉₀ of 7.3 nM across all HIV-1 strains tested^[2].
DPC-681 maintains potent activity against recombinant mutant HIV-1 variants in MT-2 cells, with no loss of potency against the D30N mutant^[2].
DPC-681 potently inhibits replication of 30 PI-resistant clinical HIV-1 isolates, with a mean IC₅₀ of 18 nM and a median IC₅₀ of 11 nM^[2].

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