Table 4. Pharmacokinetic Data of 13 in Rats and Dogs.

	iv				po				in vitro
species	CL [CLunbound]c (L/h/kg)	%Qd	t1/2e (h)	Vssf (L/kg)	AUC0-inf [AUCunbound]g (μM·h)	Cmaxh (μM)	tmaxi (h)	Fj (%)	fuk
rata	3.19 [31.6]	97	0.653	2.22	7.06 [0.713]	5.88 [0.593]	0.50	44.6	0.098
dogb	1.41 [14.5]	76	1.84	1.60	3.19 [0.309]	1.24 [0.120]	1.67	46.2	0.089

^aBased on an intravenous (iv) dose of 1 mg/kg and a per os (po) dose of 25 mg/kg in male Sprague–Dawley rats. Compound 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.

^bBased on an intravenous (iv) dose of 1 mg/kg and a per os (po) dose of 5 mg/kg in male beagle dogs. Compound was formulated in 5:25:70 DMA/PEG400/20% SBECD for iv dosing and in 0.5% methyl cellulose for po dosing.

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

^dQ = percent of liver blood flow, based on 3.3 L/h/kg (rat) and 1.85 L/h/kg (dog).

^ePlasma half-life.

^fV_ss = volume of distribution at steady state.

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

^hMaximum plasma concentration achieved.

ⁱTime at which maximum plasma concentration was achieved.

^jOral bioavailability.

^kf_u = fraction unbound to plasma protein.