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. 2020 Jul 6;11(8):1581–1587. doi: 10.1021/acsmedchemlett.0c00247

Table 2. Characterization of Compounds 21 and 26.

graphic file with name ml0c00247_0007.jpg

compound 21 26
MW, cLogP, ChromLogD 350.4; 2.88; 4.24 366.4; 1.41; 2.53
AMP permeability (nM/s) 440 266
CLND solubility (μg/mL) 137 >177
HSA binding (%) 89 79
h PBMC pIC50 (MCP-1) 8.2  
h whole blood pIC50 (MCP-1) 6.7 6.1
hepatocyte Cli (rat, human, mL/min/g tissue) 2.48; 1.42 <0.8; <0.45
rat PK (n = 1, 1 mg/kg IV) CL (mL/min/kg) (% LBF) 90 (>100%) 74 (65%)
  Clrenal (mL/min/kg) 0.2 23
  Vss (L/kg) 2.3 1.4
  T1/2 (h) 0.4 0.4
rat PK (n = 3, 3 mg/kg po) Fpo (%)   2