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C0424 Sigma-Aldrich

PK 11195

Synonym: 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide

  • CAS Number 85532-75-8

  • Empirical Formula (Hill Notation) C21H21ClN2O

  • Molecular Weight 352.86

  •  MDL number MFCD00069334

  •  PubChem Substance ID 24278822

  •  NACRES NA.77

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Properties

Related Categories Benzodiazepines and Anxiolytics, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
Quality Level   200
SMILES string   CCC(C)N(C)C(=O)c1cc2ccccc2c(n1)-c3ccccc3Cl
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
Gene Information   human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)

Description

Application

PK 11195 has been used as an inhibitor of peripheral benzodiazepine receptor (PBR) homologs in primitive erythrocytes of embryos and in osteosarcoma cytoplasmic hydrids. It has also been used as an unlabelled competitive binder in in vitro autoradiography experiments in cardiac tissue sections.

Packaging

10 mg in poly bottle

50 mg in glass bottle

Biochem/physiol Actions

PK 11195 is a peripheral benzodiazepine antagonist. It is also an antagonist for human constitutive androstane receptor (hCAR) and human pregnane X receptor (PXR). In human primary hepatocytes, PK 11195 upon demethylation elicits agonist functionality towards the receptor hCAR. PK 11195 also antagonise B-cell lymphoma 2 (Bcl-2) and may serve as a potential compound for mitochondrial targeting therapies and in the treatment of cholangiocarcinoma.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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