Table 1. Platelet-related properties of the four diastereomers of compound 1.
Diastereomer number and configuration | Platelet Aggregation (IC50, µM, 95% CI) | P2Y12 VASPa Phosphorylation (% inhibition at 10 µM, 95% CI, n = 3) | P2Y1 Calcium Flux (% inhibition at 10 µM, 95% CI, n = 6) |
1.1, SPSP | 0.15 (0.09 to 0.24) | 97.4 (42.2 to 152.7) | 73.2 (58.5 to 87.8) |
1.2, SPsRP≡SPrRP | 0.50 (0.32 to 0.79)b , e | 24.3 (−17.2 to 65.9)c | 85.7 (75.1 to 96.3) |
1.3, SPrRP≡SPsRP | 0.24 (0.14 to 0.40) | 81.2 (−8.4 to 170.8) | 59 (48.5 to 69.5) |
1.4, RPRP | 0.82 (0.45 to 1.50)e | 12.8 (−17.3 to 42.9)d | 38.9 (24.1 to 53.6)e |
VASP, vasodilator-stimulated phosphoprotein.
All comparisons vs. diastereomer 1.1.
p<0.05.
p<0.01.
p<0.001.