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Hlavní dokumenty

C0424

Sigma-Aldrich

PK 11195

Synonyma:

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

Přihlásitk zobrazení cen stanovených pro organizaci a smluvních cen


About This Item

Empirický vzorec (Hillův zápis):
C21H21ClN2O
Číslo CAS:
Molekulová hmotnost:
352.86
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

form

powder

Quality Level

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

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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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Lot/Batch Number

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Gene Expression Patterns, 9(2), 114-121 (2009)
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The optimization of translocator protein (TSPO) ligands for Positron Emission Tomography as well as for the modulation of neurosteroids is a critical necessity for the development of TSPO-based diagnostics and therapeutics of neuropsychiatrics and neurodegenerative disorders. Structural hints on the
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Alterations of 'peripheral-type' benzodiazepine receptors (PTBRs) in brain are a feature of hepatic encephalopathy (HE). Although ammonia toxicity has been implicated in the disorder, recent findings suggest an accumulation of manganese in the brains of cirrhotic patients dying in hepatic

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