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. Author manuscript; available in PMC: 2012 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2010 Oct 30;19(1):613–622. doi: 10.1016/j.bmc.2010.10.052

Table 3.

In vitro Pharmacokinetic Assays of 1a

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Aqueous Solubility Maximum Solubility (μM)
56
Caco-2 Permeability Papp (A→B) (10−6 cm/s) Papp (B→A) (10−6 cm/s) Ratio (B→A/A→B)
4.7 0.46 0.1
PBS/Mouse Plasma Stability Plasma T1/2 (min) PBS Amount Remaining at 60 min (%) Recovery Plasma vs. PBS (%)
16 100 91
Microsomal Stability (human) CL’int (mL/min/kg) T1/2 (min) CL’int No NADPH (mL/min/kg)
58.5 39 16.2
Microsomal Stability (mouse) 292 13 61.2