. Author manuscript; available in PMC: 2018 May 11.

Published in final edited form as: J Med Chem. 2017 Apr 25;60(9):3979–4001. doi: 10.1021/acs.jmedchem.7b00271

Table 6.

ADME properties of selected 15-PGDH inhibitors

Compound:	(+)-1	(R)-12q	(S)-12q	12w	32	44c
In Vitro
mouse S9 (t_1/2, min)	13 (83)^a	35	289	>240	83	91
human S9 (t_1/2, min)		>240	224
plasma protein binding (mouse, %)	99.98^a	78		56	99	90
In Vivo (mouse, 10 mg/kg IP)
C_max (μM)	1.6 (1.5)^a	3.1		6.2	13.0	10.6
C_3h (μM)^b	0.13 (0.26)^a	<0.01		0.06	4.2	0.06
AUC (min*μg/mL)	43 (83)^a	47		116	959	172

Data from racemic compound.

Plasma concentration 3h after dose.