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 | |
See Supporting Information for experimental details