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. Author manuscript; available in PMC: 2012 Feb 23.
Published in final edited form as: J Med Chem. 2010 Oct 14;53(19):7067–7075. doi: 10.1021/jm100691c

Table 5.

Pharmacokinetic Screening Resultsa

Compound Cmax (nM) Tmax (min) t1/2 (min) AUCt (×104nM·min)
AUDAb 14 80 126 0.3
2 138 45 78 1.9
3 2,770 60 50 35
4 4,600 50 56 58
12 5,570 30 72 92
13 4,810 30 56 74
14 5,860 50 58 95
15 13,000 70 82 283
24 8,410 83 378 467
25 18,300 188 381 1,360
27 3,790 440 881 375
35 5,940 230 814 516
40 17400 220 980 1400
52 8900 190 1180 985
a

Values are from single oral cassette dosing at 5 mg/kg in 120-150 μl of 20% PEG400 v/v in oleic ester rich triglyceride

b

Full pharmacokinetic profiles are shown in Figures S1 – S3 and plots of murine AUC as a function of the IC50 on the human enzyme and the murine enzyme are shown if Figures S4 and S5 in the supplementary material.

c

AUDA gave biphasic kinetics