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. Author manuscript; available in PMC: 2023 Apr 28.
Published in final edited form as: J Med Chem. 2022 Apr 18;65(8):6287–6312. doi: 10.1021/acs.jmedchem.2c00195

Table 5.

In Vivo PK Profile in CD-1 Micea

3 mg/kg iv
 10 mg/kg po
compnd CL (mL/min/kg) AUC0,inf (h·ng/mL) Vss (L/kg) Cmax (ng/mL) AUC0,inf (h·ng/mL) t1/2 (h) F%
1 b 78 642 16 n.c. n.c. n.c. n.c.
34 118 429 3.8 279 397 1.2 28
36 41 1240 1.6 652 508 1.4 12
37 25 2075 1.1 1083 1000 1.2 15
38 76 707 2.3 2013 1712 1.2 73
40 20 2570 0.7 2767 3626 1.2 42
41 26 1951 1.6 2083 3984 1.3 61
a

Pharmacokinetic parameter values represent the average of three animals.

b

The iv PK parameter values are for one surviving animal due to the lethality of 1. The oral exposure of 1 was below the limit of quantitation when administered orally at 3 mg/kg. Not calculated = n.c.