CAS: 179461-52-0

PD 151746

PD 151746 is a small molecule that binds to calcium and inhibits the activity of mitochondrial membrane potential, resulting in cytosolic calcium overload and neuronal death. PD 151746 binds to both the extracellular domain of the α-subunit of voltage-gated L-type calcium channels (L1CAM) and the intracellular domain of the α-subunit of voltage-gated T-type calcium channels (T1CAM). It has been shown to inhibit both physiological functions and antimicrobial peptides, such as CAMP, through irreversible inhibition. PD 151746 has also been shown to be an effective treatment for autoimmune diseases, including multiple sclerosis.

Applications PD 151746 acts as a cell-permeable calpain inhibitor which induce pertussis toxin (PTx)-sensitive chemotaxis in neutrophils and human monocytes. This results in an inhibition of inflammation. References Fujita, H. et al.: Arch. Biochem. Biophys., 513, 51 (2011);

PD151746: calpain inhibitor, Ki μ-calpain=0.26μM, Ki m-calpain=5.33μM; reduces oxLDL cytotoxicity.