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. Author manuscript; available in PMC: 2021 Mar 24.
Published in final edited form as: J Med Chem. 2020 Apr 22;63(10):5242–5256. doi: 10.1021/acs.jmedchem.0c00035

Table 6.

In Vivo PK Profiles of Compounds 44 and 45 in Ratsa

44 45
i.v. (10 mg/kg) bt1/2 (h) 3.5 ± 0.71 4.1 ± 0.43
cCmax (ng/mL) 2861 ± 426 2090 ± 265
dAUC0-t (ng·h/mL) 6763 ± 590 7033 ± 2161
eCL (L/h/kg) 1.48 ± 0.13 1.48 ± 0.38
p.o. (20 mg/kg) t1/2 (h) 2.4 ± 0.55 2.8 ± 0.27
Cmax (ng/mL) 575.1 ± 179 605.5 ± 182
AUC0-t (ng·h/mL) 5171 ± 3447 4966 ± 1772
fF (%) 38.2 35.3
a

Compounds were formulated in 10%DMSO/60%PEG400/30% Saline and administrated intravenously (i.v.) or per os (p.o.).

b

t1/2, half-life.

c

Cmax, maximum plasma concentration achieved.

d

AUC0‑t, total exposure following a single dose.

e

CL, total clearance.

f

F, oral bioavailability.