Table 8.
Differences in Potency between Enantiomers Extended to Metabolic Stability
Compound | ![]() |
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|||
---|---|---|---|---|---|---|
NF54 EC50 (nM) | 27 | >5000 | 9.2 | |||
Liver Microsomesaa | CLint | t1/2 (min) | CLint | t1/2 (min) | CLint | t1/2 (min) |
Mouse | Med | 26.5 | Low | 103 | High | 1.8 |
Human | Med | 9.9 | Low | 95 | High | 1.2 |
intrinsic clearance in liver microsomes; where high clearance corresponds to low stability in the presence of liver enzymes