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. 2016 Feb 16;7(4):351–356. doi: 10.1021/acsmedchemlett.6b00005

Table 4. Preclinical Species Hepatocyte Stability and in Vivo Pharmacokinetic Data for 16.

graphic file with name ml-2016-00005n_0007.jpg

    IV (1 mg/kg)b
POc
Species liver microsomes Clhep (mL/min/kg)a in vivo Cl (mL/min/kg) Vss (L/kg) Dose (mg/kg) AUC (μM·h) F% PPB%
Mouse 19 17 1.7 25 47 75 78
Rat 14 28 3.2 5 8.3 77 71
a

Hepatic clearance was predicted from liver microsomes incubations using the “in vitro t1/2 method.”9

b

Male Sprague–Dawley rats or female CD-1 mice were dosed intravenously with 1 mg/kg of 16 prepared in 60% PEG400/10% ethanol.

c

Compound 16 was administered PO at the indicated dose in 0.5% methylcellulose with 0.2% Tween 80 (MCT).