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JNJ-47965567 is a potent and selective P2X7 antagonist (pIC50 values are 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively). Selective over a panel of 50 other receptors, ion channels and transporters. JNJ-47965567 reduces BzATP-induced IL-1β release from monocytes in vitro and from rat brain in vivo. JNJ-47965567 attenuates amphetamine-induced hyperactivity in rats. Brain penetrant.
| Cell Experiment | |
|---|---|
| Cell lines | Hela and SiHa cells |
| Preparation method | Lactate dehydrogenase (LDH) test kit was used to assess thecytotoxicity of atractylenolide Iand in combination with or without 100 μM BzATP or 20 μM JNJ47965567. Cells were cultured in 96-well plates (6 × 10^3 cells/well). After treatment with the designed concentrations of drugs, cell culture supernatant was transferred to the new 96-well plate for LDH analysis. |
| Concentrations | 20 μM |
| Incubation time | 24 h ~ 72 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J |
| Formulation | DMSO (10%) and PEG400 (90%) |
| Dosages | 30 mg/kg/day (5 Days) |
| Administration | Intraperitoneal injection |
| Molecular Weight | 488.64 |
| Formula | C28H32N4O2S |
| CAS Number | 1428327-31-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 80 mg/mL 1eq. HCl 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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