1-Oleoyl-2-acetyl-sn-glycerol

1-Oleoyl-2-acetyl-sn-glycerol (CAS No.: 86390-77-4) is a synthetic, cell-permeable analog of the endogenous second messenger diacylglycerol (DAG) and is widely used as a pharmacological activator of protein kinase C (PKC), a family of serine/threonine kinases that regulate diverse cellular processes through phosphorylation-dependent signaling pathways. By mimicking DAG, this compound directly engages PKC isoforms and modulates downstream signaling cascades involved in calcium-dependent signal transduction, membrane dynamics, and gene expression. In cellular systems, it has been shown to influence ion channel activity, including reversible inhibition of voltage-dependent calcium currents in pituitary and neuronal cell models at low to mid micromolar concentrations, as well as activation of transient receptor potential canonical (TRPC) channels leading to increased intracellular calcium influx. Additional reported effects include stimulation of reactive oxygen species generation in neutrophils, enhancement of phosphoinositide metabolism in platelets, and modulation of secretory and proliferative responses in various cell types. It can also attenuate receptor-mediated proton secretion in gastric parietal cells, reflecting its broader impact on PKC-regulated physiological processes. Following cellular uptake, it may be metabolized into phosphatidic acid derivatives, further contributing to lipid-mediated signaling networks. This compound is commonly applied in biochemical and cell-based assays to investigate PKC-dependent mechanisms, calcium signaling, and lipid-mediated pathways, with experimental concentrations typically selected in the micromolar range depending on the model system and study objectives.