Table 4. A-Ring SARs on Oxygen Affinity with Purified HbS and Whole Blood and on the Change in Delay Time to the Onset of Polymerization, and PK Properties in Rats.
a
Data expressed as Δp50%: the % change from baseline of pO2 at which HbS (at 25 μM) is 50% saturated with O2 in the presence of test compound at 30 μM.
b
Data expressed as Δp50%: the % change from baseline of pO2 at which whole blood (at 20% hematocrit, 1 mM) is 50% saturated with O2 in the presence of test compound at 1 mM.
c
Data expressed as ΔT%: the % change from baseline of delay time of HbS at 50 μM in the presence of test compound at 75 μM.
d
Not determined.
e
Tested at 500 μM.
f
AUC(0-∞) value normalized by PO dose [(ng·h/mL)/(mg/kg)]. Please see Supporting Information for standard deviation and number of tests.