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. Author manuscript; available in PMC: 2013 Jul 11.
Published in final edited form as: J Med Chem. 2008 Oct 4;51(21):6642–6645. doi: 10.1021/jm800986w

Table 2.

Data for Pharmacokinetics in Vitro and in Vivo

in vivo rat PKc (i.v., 1 mg/kg; p.o., 2 mg/kg)
cmpd CYP-450sa
% inh. at
10 µM		 HLMS at 2 mg/mL
T1/2 (min)b 		Cl (i.v.)
mL/min/kg		 T1/2
(iv) h		 Vd (i.v.)
L/kg		 AUC (i.v.)
µM-h		 Cmax (p.o.)
µM		 F (%)
1 96/94/80/90 18 181 0.4 3.7 0.3 0.0 0
2 64/33/51/23 6 161 0.5 5.3 0.3 0.0 0
3 87/40/1/20 20 18 2.2 1.9 2.8 0.02 0.3
4 93/79/36/92 15 11 2.6 1.0 4.3 0.12 0.4
5 80/75/0/46 35 61 0.8 3.0 0.7 0.05 7.0
a

CYP-450s: 2C9/2D6/3A4/1A2.

b

HLMS: human liver microsomal stability.

c

Data reported is the mean of 3 determinations, and the standard error is within 30% of the mean except for Cmax, which is within 50%.