Table 6. Pharmacokinetic Properties of 5.

Part A
	Compound 5
Metabolic Stability after Incubation with Liver Microsomes
Mouse CLblood [L/h/kg]/Fmax [%]	0.19/96
Rat CLblood [L/h/kg]/Fmax [%]	0.15/96
Dog CLblood [L/h/kg]/Fmax [%]	<0.001/100
Human CLblood [L/h/kg]/Fmax [%]	<0.001/100
Metabolic Stability after Incubation with Hepatocytes
Rat CLblood [L/h/kg]/Fmax [%]	3.8/9.4
Dog CLblood [L/h/kg]/Fmax [%]	1.5/28
Permeability in Caco2 Monolayer Cells
Caco2 Papp(A-B) [nm/s]/Papp (B-A) [nm/s]/ratio	106/204/1.9
Plasma Protein Binding (Fraction Unbound)
NMRI mouse female [%]	0.58
Caucasian human (mixed gender) [%]	4.3

Part B
species	CLblood[L/h/kg]	Vss [L/kg]	t1/2[h] i.v.	AUC [mg·h/L]i.v.	AUC [mg·h/L] p.o.	F [%] p.o.	Cb/Cp
rat	0.73	1.5	10	1.0	1.5	73	0.52