C0424

PK 11195

peripheral benzodiazepine antagonist, powder

• Synonym(s): 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
• Empirical Formula (Hill Notation): C₂₁H₂₁ClN₂O
• CAS Number: 85532-75-8
• Molecular Weight: 352.86
• UNSPSC Code: 12352200
• PubChem Substance ID: 24278822
• NACRES: NA.77
• MDL number: MFCD00069334
• Form: powder

Properties

• Product Name: PK 11195,
• form: powder
• Quality Segment: 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.

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable