Table 1

In vitro clearance and in vivo duration of methyl branch and methylene analogs

Table 1

Structure		In Vitro		In Vivo
Structure		V_max^1-a	K_M^b	CL_int^1-c	CL_p^d	t_1/2^1-e
1		1.2 ± 0.2^1-f	1600 ± 420	0.77	14	0.4
2		3.6 ± 0.3	770 ± 90	4.6	58	0.2
3		3.3 ± 0.4	600 ± 60	5.5	5.8	0.8
4		3.4 ± 0.6	200 ± 40	17	16	0.3
5		1.0 ± 0.1	1500 ± 130	0.69	4.5	1.4
6		5.3 ± 1.2	2500 ± 600	2.1	14	0.3

↵1-a V_max(nmol/min/mg protein).
1-b K_M (μM).
↵1-c CL_int is theV_max/K_M ratio defined as μl/min/mg protein.
1-d CL_p (ml/min/kg) is defined as k_el * V_d .
↵1-e t_1/2 (hr) is plasma half-life. Intravenous doses are 20 mg/kg.
↵1-f ±SD (N = 5 determinations).