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. 2020 Jan 27;11(2):188–194. doi: 10.1021/acsmedchemlett.9b00578

Table 4. Pharmacokinetic Parameters of 13 and 26 in Sprague Dawley Rat Dosed at 1 mg/kg IV (Parent Compound) and 3 mg/kg PO (Ethyl Ester Prodrug)a.

Administered Compound Route oral Cmax (nM) AUC(0–7) (nM·Hours) CL (mL/min/kg) Vdss (L/kg) Elimination t1/2 (IV) (Hours) %F
13 (active) IV   8730 5 0.1 0.8  
36 (prodrug) PO 12600 10100       42
26 (active) IV   8100 5 0.1 1.0  
39 (prodrug) PO 5380 5630       25
a

36 is the ethyl ester prodrug of 13; 39 is the ethyl ester prodrug of 26.