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DO264 is a potent selective, and in vivo active ABHD12 inhibitor, with an IC50 of 11 nM. DO264 augments inflammatory cytokine production from human THP-1 macrophage cells. DO264 blocks lyso-PS hydrolysis activities of recombinant mouse and human ABHD12 in transfected HEK293T cell lysates (DO264 IC50 values of ~30 and 90 nM against mouse and human ABHD12, respectively) and the ABHD12-dependent lyso-PS lipase activity of membrane lysates from mouse brain (IC50=2.8 nM, 2.4 nM-3.3 nM) and human THP-1 cells (IC50= 8.6 nM, 6.3 nM-12 nM). In vivo, Mice treated with DO-264 display dose-dependent increases in brain lyso-PS and 20:4 PS content that are qualitatively similar to the changes observed in ABHD12–/– mice.
| Molecular Weight | 558.40 |
| Formula | C23H20Cl2F3N5O2S |
| CAS Number | 2301866-59-9 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage | -20°C, dry, protect from light, sealed |
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