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. 2015 Mar 6;6(4):461–465. doi: 10.1021/acsmedchemlett.5b00010

Table 4. Rat PK Profiles and Plasma Protein Binding Data in Human and Rat Plasma (10%)a.

compd F% Clp (mL/min/kg) Vdss (L/kg) T1/2 (h) AUCNpo (μM·h·kg/mg) free fraction in 10% plasma (%, human, rat)
2a 15 47 4.6 1.5 0.11 0.2, 1
2d 36 33 3.4 1.7 0.33 0.2, 0.7
2f 6 32 1.8 1.6 0.067 3.4, 6.4
2m 27 19 1.6 1.8 0.49 4, 1.7
2o 54 20 1.9 1.2 0.79 -
2p 44 67 2.3 0.69 0.07 9.3, 6.5
2q 11 80 5.0 0.94 0.046 0.2, 0.8
3c 44 23 3.4 2.4 0.067 0.2, 0.5
3e 15 55 3.2 1.2 0.085 5.8, 6.4
a

Values are an average of two wistar han rats for IV dose and three rats for p.o. dose. Formulation: The IV doses were formulated at 1 mg/kg in DMSO/PEG200/water (10:60:30), and the oral doses were formulated at 2 mg/kg in imwitor/tween (1:1) and given by oral gavage. F%, oral bioavailability; Clp, plasma clearance; Vdss, volume of distribution; Cmax, observed maximal plasma concentration following oral dosing; T1/2, terminal half-life; AUCNpo; normalized area under the curve for oral dosing.