An isoquinoline carboxamide that acts as a potent ligand for peripheral bezodiazepine receptor (Kd = 20nM). 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 (˜100uM).
Synonyms:TSPO Activator II, Mitochondrial Translocator Protein Activator II, PK 11195, PK-11195, PK11195
Molecular Formula:C₂₁H₂₁ClN₂O
Solubility:DMSO
Primary Target:peripheral bezodiazepine receptor
Primary Target Ki:20nM
Molecular Weight:352.86
Appearance:Supplied as a white solid.
Purity:≥98% (HPLC)
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
