Merck, 5059810001, PK11195

General description
An isoquinoline carboxamide that acts as a potent ligand for peripheral bezodiazepine receptor (Kd = 20 nM). Exhibits anti-inflammatory properties. Binds to monocytes and following lesioning its binding up-regulated in brain macrophages and activated microglia. Shown to enhance the susceptibility of cells to apoptosis induction by DNA damaging agents and can reverse the suppression of apoptosis by Bcl-2. Serves as a ligand of the outer membrane translocator protein and reduces mitochondrial transmembrane potential within 30 minutes of exposure (˜100 µM).
Biochem/physiol Actions
Primary Target
peripheral bezodiazepine receptor
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Naoi, M., et al., 2013. J. Neural Transm.In press
Casellas, P., et al., 2002. Neurochem. Int.40, 475.
Waterfield, J.D., et al., 1999. Rheumtology38, 1068.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)