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. Author manuscript; available in PMC: 2012 Apr 28.
Published in final edited form as: J Med Chem. 2011 Apr 5;54(8):3037–3050. doi: 10.1021/jm2001376

Table 2.

PK Parameters of the Compounds 21b,e–j in Mice by Oral Cassette Dosing at 5 mg/kg (n =1) and in Rats by Oral Administration at 1 mg/kg (n=4).

species Inhibitors Tmax (h) Cmax (nM) AUC (nM*h) t1/2 (h)
Mouse 21h 0.8 190 375 2.4
21i 0.8 260 980 2.6
21j 0.8 290 1335 2.4
21e 0.5 100 125 3.1
21b 0.5 19 35 1.0
21g 0.5 42 100 3.5
21f 0.5 20 22 1.7

Rat 21i 1.5 ± 0.6 415 ± 139 2764 ± 804 13 ± 4
21j 1.0 ± 0.7 180 ± 71 1230 ± 521 12 ± 6