C0424

PK 11195

• Synonyme(s) : 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
• Formule empirique (notation de Hill) : C₂₁H₂₁ClN₂O
• CAS Number: 85532-75-8
• Poids moléculaire : 352.86
• Numéro MDL: MFCD00069334
• Code UNSPSC : 12352200
• ID de substance PubChem : 24278822
• Nomenclature NACRES : NA.77

Propriétés

• Forme: powder
• Niveau de qualité: 200
• Chaîne SMILES: 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
• Clé InChI: RAVIZVQZGXBOQO-UHFFFAOYSA-N
• Informations sur le gène: 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.

Actions biochimiques/physiologiques

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable