5.05981

PK11195

• Synonym(s): PK11195, TSPO Activator II, Mitochondrial Translocator Protein Activator II, PK 11195, PK-11195, PK11195
• Empirical Formula (Hill Notation): C₂₁H₂₁ClN₂O
• CAS Number: 85532-75-8
• Molecular Weight: 352.86
• MDL number: MFCD00069334
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• potency: 20 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mM
• storage temp.: 2-8°C
• InChI: 1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
• InChI key: RAVIZVQZGXBOQO-UHFFFAOYSA-N

Description

General description

An isoquinoline carboxamide that acts as a potent ligand for peripheral bezodiazepine receptor (K_d = 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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable