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. Author manuscript; available in PMC: 2024 Sep 30.
Published in final edited form as: J Med Chem. 2024 May 24;67(11):9709–9730. doi: 10.1021/acs.jmedchem.4c00856

Table 6.

In Vivo PK Profiles of Compounds 15b or 24f Following 20 mg/kg Oral and 10 mg/kg Intravenous Dosing in Ratsa

route AUC0−∞ (ng h/mL) t1/2 (h) Tmax (h) Cmax (ng/mL) CL (L/h/kg) Vss (L/kg) F (%)
15b PO 3535 ± 1411 1.1 ± 0.02 0.5 2212 ± 587 6.2 ± 2.1 9.6 ± 3.2 37.6 ± 15
15b IV 4679 ± 1280 0.6 ± 0.2 6456 ± 988 2.3 ± 0.7 1.8 ± 0.1
24f PO 662 ± 191 3.3 ± 1.5 1.0 192 ± 109 nd nd 7.0 ± 2.0
24f IV 4746 ± 268 0.7 ± 0.3 13733 ± 1358 35.2 ± 2.0 0.55 ± 0.08
a

Values are mean ± SD from n = 3 biological replicates.

Cmax, maximum concentration of drug in plasma; Tmax, time to maximum concentration of drug in plasma; AUC, area under the curve (t = 0 to 24 h); Vss, volume of distribution at steady state; CL, plasma clearance; t1/2, terminal half-life; F, absolute oral bioavailability; nd, not determined. Formulation for PO and IV: DMSO:20% HP-β-CD in saline = 1:9.