Table 2

In vitro blood cell association and stability of [125I]SB-251353

GROβ-TRANTESTime at 37°CBlood/Plasma Conc. Ratio2-a2-bPercent Cell Association2-a2-cPercent TCA Precipitable2-d
ng/ml μg/ml min
50002-e 0.875 (0.020)21.67 (5.10)87.0
2502-e 0.616* N.D.N.D.
0100.827 (0.028)16.72 (0.70)N.D.
0600.739 (0.040)17.42 (2.87)88.6
25,000002-e 0.617 (0.031)1.69 (0.55)N.D.
0100.589 (0.013)1.27 (0.21)N.D.
0600.592 (0.040)1.86 (0.26)N.D.
  • 2-a  Mean (standard deviation);n = 3 except for * where n = 2 (no standard deviation reported).

  • 2-b  Hematocrit of pooled mouse whole blood was 0.43.

  • 2-c  Radioactivity remaining in the cell pellet after three sequential phosphate-buffered saline washes.

  • 2-d  Percentage of radioactivity in plasma, pooled from whole blood incubation, that was trichloroacetic acid (TCA) precipitable (N.D. indicates no data).

  • 2-e  Incubation performed on wet ice (∼4°C).