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. 2022 Sep 1;13(10):1634–1641. doi: 10.1021/acsmedchemlett.2c00310

Table 5. Pharmacokinetic Properties of Compounds in Ratsa.

graphic file with name ml2c00310_0013.jpg

compound metabolic stability rat/human (%)b CLtot (mL/min/kg)c Vdss (L/kg) t1/2 (h) F (%)c serum fu (%) solubility (μM) pH 1.2/pH 6.8/pH 6.8 with TCA EPSAd
2 29/3 6.8 0.1 0.7 ND 1.1 ND/ND/26 113
11 53/18 11.4 0.8 1.6 ND 0.1 ND/ND/NT 88
15 60/20 5.7 0.7 2.0 0.2 0.1 ND/ND/NT 93
16 63/23 8.2 1.9 3.9 3.3 0.1 ND/ND/10 92
a

ND: not detected; NT: not tested.

b

Metabolic stability using human and rat hepatic microsomes.

c

All compounds were administered to rats by intravenous administration at 1 μmol/kg solution and oral administration at 2 μmol/kg suspension.

d

Exposed polar surface area (EPSA) analysis by supercritical fluid chromatography.