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. Author manuscript; available in PMC: 2023 Sep 9.
Published in final edited form as: J Med Chem. 2023 Feb 24;66(5):3372–3392. doi: 10.1021/acs.jmedchem.2c01858

Table 6.

In Vitro Metabolic Stability Of Class I, II, and III in Mouse Liver Microsomes (MLM)

DMPK (MLM)a
DMPK (MLM)a
ID T1/2 (min) CLint (mL/min/mg) ID T1/2 (min) CLint (mL/min/mg)
Class I 27b 41.77 1.66 35b 45.00 1.5
27c 39.94 1.735 35c 23.66 2.93
31h 7.70 8.90 Class III 35d 49.46 1.4
31i 23.44 2.96 35g 22.60 3.1
31j 14.60 4.70 35h 105.00 0.66
31l 55.00 1.30 35i 120.60 0.60
Class II 31o 50.15 1.40
31q 12.63 5.5
32a 13.29 5.2 8 22 Antagonist 12.35 5.614
32c 53.71 1.29 1 Antagonist 10.04b 86.316
32d 35.46 1.96 6 Agonist 360.00 1.416
a

Compounds were incubated with MLM and cofactors for phases I and II, as described in the Experimental Section.

b

T1/2 (h) as previously reported.19,20