Table 5. In vitro DMPK profile for 3 and pharmacokinetic parameters for 3 in rats.^a.

Sol.b,c	CLhep HH/MH/RHc,d	Papp/MDR1c,e	rPPBf
121	13/65/36	2.1/47	98.9 ± 1.1

dose (mpk, route)	Cmax (μM)	Tmax (h)	AUC0-inf (μM·h)	T1/2 (h)	CLp (mL/min/kg)	Vss (L/kg)
1, iv	2.9 ± 0.2	N/A	0.18 ± 0.01	0.13 ± 0.01	177 ± 12	1.4 ± 0.1
20, ip	5.3 ± 1.7	0.06 ± 0.04	13.5 ± 0.0	2.2 ± 0.5	N/A	N/A

^aRat PK data is mean ± SD.

^bKinetic solubility (μM) at pH 7.2.

^cSD not applicable.

^dPredicted hepatic clearance (mL/min/kg).

^eApparent permeability (10^–6 cm/s), apical to basolateral side (A to B), and MDR1 efflux ratio.

^fPlasma protein binding in rat ± SD.