TABLE 5.
Comparative biophysical properties of SCH-C and vicriviroc
| Assay | SCH-C | Vicriviroc |
|---|---|---|
| Protein binding (human plasma) | 16% free (3%) | 16% free (3.5%) |
| hERG (IC50) | 1.1 μMa | 5.8 μM |
| CYP 450 enzyme inhibition (IC50) | >30 μM | >30 μM |
a
Concentration-response curve analysis for hERG activity by nonlinear regression of all data points: 0.11, 0.3, and 1.1 μM SCH-C resulted in an IC50 of 1.1 μM (95% CI, 0.6 to 1.9 μM); 1, 3, and 10 μM vicriviroc revealed an IC50 of 5.8 μM (95% CI, 4.7 to 7.2 μM). n = 4 to 5 replicates per drug concentration, and n = 5 to 7 per vehicle control group.