TABLE 1.

Comparison of GS-9131 metabolism in different lymphoid cell types

Cell typeExtracellular concn of GS-9131 (μM)aIntracellular concn ± SD (pmol/million cells)b
GS-9148GS-9148-MPGS-9148-DP
CEM-CCRF1.09.18 ± 1.992.70 ± 0.336.60 ± 1.00
Quiescent PBMCs1.07.92 ± 1.352.07 ± 0.903.90 ± 0.55
Activated PBMCs1.011.6 ± 7.73.95 ± 2.635.64 ± 2.42
Activated CD4+0.31.70 ± 0.340.14 ± 0.011.50 ± 0.17
  • a Cells were incubated for 24 h at the indicated concentrations.

  • b Values represent the means ± standard deviations (SD) from two to three independent experiments done in duplicate. Quiescent and activated PBMC experiments were done with cells isolated from single donors, while activated CD4+ cell experiments were done with cells pooled from four donors.