Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| HEK293 | IC50 | 0.75 μM | Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay | [PMID: 30528164] |
| Peritoneal macrophage | IC50 | 0.723 μM | Antiinflammatory activity in LPS/IFNgamma-differentiated Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 15 mins followed by ATP/LPS challenge measured after 30 mins by sandwich ELISA | [PMID: 29133043] |
| Peritoneal macrophage | CC50 | 325.4 μM | Cytotoxicity against Swiss Webster mouse peritoneal macrophages by LDH release assay | [PMID: 29133043] |
| THP-1 | IC50 | 0.689 μM | Antiinflammatory activity in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA | [PMID: 29133043] |
| THP-1 | IC50 | 156 nM | Antagonist activity at human recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay | [PMID: 19540765] |