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. 2018 Jun 23;9(7):594–599. doi: 10.1021/acsmedchemlett.7b00505

Table 3. Profiling of Compound 31a.

solubility (pH = 7.4) (μM) 98
Caco-2 Papp (10–6 cm/s) 18.8
human hepatocytes Clint (μL/min/10–6 cells) 1.7
sPLA2-X IC50 (μM) 0.026
sPLA2-X mouse IC50 (μM) 0.096
sPLA2-IIa IC50 (μM) 0.31
sPLA2-V IC50 (μM) 2.23
pharmacokinetics rat dog
dose i.v./p.o. (μmol/kg) 1/4 1/–
CL (mL/min/kg) 9.1 0.75
AUC (μM·h) 1.84/11 8.78/–
Vdss (L/kg) 2.54 0.44
F (%) 100  
a

See Supporting Information for experimental details