Table 3. Mouse Pharmacokinetic Profiles for Fluorinated Analogues 12 and 13^a.

	iv				po				in vitro
compound	CL [CLunbound]d (L/h/kg)	%Qe	t1/2f (h)	Vssg (L/kg)	AUC0-inf [AUCunbound]h (μM·h)	Cmaxi [Cmax-unbound] (μM)	tmaxj (h)	Fk (%)	ful
12b	4.45 [202.3]	82	0.402	1.10	42.01 [0.924]	52.14 [1.15]	0.250	91.6	0.022
13c	2.16 [102.9]	40	1.63	1.36	88.88 [1.87]	67.36 [1.41]	-	100	0.021

^aBased on an intravenous (iv) dose of 1 mg/kg and a per os (po) dose of 100 mg/kg in fasted male Balb/C mice (except where indicated).

^bCompound was formulated in 5:25:70 DMA/PEG400/20% SBECD for iv dosing and in 0.5% methyl cellulose (adjusted to pH 3) for po dosing.

^cCompound was formulated in 5:60:35 DMA/PEG400/20% SBECD for iv dosing and in 0.5% methyl cellulose (adjusted to pH 3–4) for po dosing.

^dCL = total clearance. CL_unbound = CL/free fraction.

^eQ = percent of liver blood flow, based on 5.4 L/h/kg (mouse).

^fPlasma half-life.

^gV_ss = volume of distribution at steady state.

^hExtrapolated total exposure following single dose. Calculated unbound exposure is in parentheses.

ⁱMaximum plasma concentration achieved.

^jTime at which maximum plasma concentration was achieved.

^kOral bioavailability.

^lf_u = fraction unbound to plasma protein.