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. 2012 Apr 23;55(9):4244–4273. doi: 10.1021/jm300041e

Table 4. Complete in Vivo Pharmacokinetic Profile of Selected Analogues in Micea.

  IV PK parameters
PO PK parameters
entry Vd(L/kg) CL (mL/min/kg) T1/2(h) AUC(0–24 h)(h·nM) Cmax(nM) Tmax(h) T1/2(h) AUC(0–24 h)(h·nM) F(%)
15 12.3 188.9 2.7 1072 235 2.0 4.20 965 15
22 10.2 49.2 2.0 4119 1538 1.0 4.35 12155 74
24 7.5 27.5 5.5 7062 1723 3.0 5.21 21058 75
27 23.7 60.0 6.2 3442 1803 1.7 8.95 17894 87
29 7.5 36.1 18.0 7607 1642 1.0 14.54 32409 107
34 2.7 12.5 2.8 16525 3651 1.0 2.71 50619 77
36 1.2 25.9 0.8 9090 6404 1.0 2.95 19447 53
a

PO dosing; dose (mg/kg), 20; species/strain, mouse, male balb/c; formulation, 2.5 mg/mL in PEG300/D5W, 3:1, solution; Vd = volume of distribution; CL = clearance; Cmax = maximal concentration; Tmax = time at maximal concentration; AUC = area under the curve; F = oral bioavailability.