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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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