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5.05981

PK11195

Synonym(s):

PK11195, TSPO Activator II, Mitochondrial Translocator Protein Activator II, PK 11195, PK-11195, PK11195

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About This Item

Empirical Formula (Hill Notation):
C21H21ClN2O
CAS Number:
85532-75-8
Molecular Weight:
352.86
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00069334
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light
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assay

≥98% (HPLC)

Quality Level

100

form

solid

potency

20 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mM

storage temp.

2-8°C

SMILES string

Clc1c(cccc1)c2nc(cc3c2cccc3)C(=O)N(C(CC)C)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

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)

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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Global Trade Item Number

SKUGTIN
505981000104055977262537