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. Author manuscript; available in PMC: 2021 Feb 13.
Published in final edited form as: J Med Chem. 2020 Jan 16;63(3):1032–1050. doi: 10.1021/acs.jmedchem.9b01218

Table 5.

Mouse liver microsomal (MLM) stability of selected novel EP2 antagonistsa

Compd. MLM T1/2 (minutes)
3a <2
8c 2.9
8d 13
8g 2.9
14a 6.5
20b 8
20c 17
20e 12
20f 96
20h 16
20o 17
24a 17
24c 26
24e 15
24i 56
a

The compounds at 1μM were incubated in 0.125 mg/mL liver microsomes that are activated with addition of NADPH (final concentration 1 mM) and quenched the reaction at 0, 5, 15, 30, 60 and 120 min using ice-cold acetonitrile. The % compound remaining was measured using LC-MS/MS from which half-life was calculated. The work was done at CRO laboratories.