PK 11195

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Cat.No. 0670 - PK 11195 | C21H21ClN2O | CAS No. 85532-75-8
Description: Antagonist at peripheral benzodiazepine receptors
Chemical Name: 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews (1)
Literature

Biological Activity

Possesses high affinity for the peripheral benzodiazepine receptor (PBR, TSPO) without binding to other known neurotransmitter receptors. Also inhibits the human constitutive androstane receptor (hCAR).

Compound Libraries

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Technical Data

M. Wt 352.86
Formula C21H21ClN2O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 85532-75-8
PubChem ID 1345
InChI Key RAVIZVQZGXBOQO-UHFFFAOYSA-N
Smiles CCC(C)N(C)C(=O)C1=NC(C2=CC=CC=C2Cl)=C2C=CC=CC2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 17.64 50
DMSO 17.64 50

Preparing Stock Solutions

The following data is based on the product molecular weight 352.86. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.67 mL 28.34 mL 56.68 mL
2.5 mM 1.13 mL 5.67 mL 11.34 mL
5 mM 0.57 mL 2.83 mL 5.67 mL
25 mM 0.11 mL 0.57 mL 1.13 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Conway et al (1998) Temporal changes in glial fibrillary acidic protein messenger RNA and [3H]PK11195 binding in relation to imidazoline-I2-receptor and α2-adrenoceptor binding in the hippocampus following transient global forebrain isch Neuroscience 82 805 PMID: 9483537

Le Fur et al (1983) Differentiation between two ligands for peripheral benzodiazpine binding sites [3H]-Ro 5-4864 and [3H]-PK11195, by thermodynamic studies. Life Sci. 33 449 PMID: 6308375

Li et al (2008) The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human androstane receptor. Mol.Pharmacol. 74 443 PMID: 18492798


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Keywords: PK 11195, PK 11195 supplier, antagonists, peripheral, benzodiazepine, receptors, GABAA, Receptors, PK11195, PBR, TSPO, Constitutive, Androstane, Receptor, Translocator, Protein, 0670, Tocris Bioscience

3 Citations for PK 11195

Citations are publications that use Tocris products. Selected citations for PK 11195 include:

Gut et al (2013) Whole-organism screening for gluconeogenesis identifies activators of fasting metabolism. J Cell Mol Med 9 97 PMID: 23201900

Sutter et al (2003) Ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in oesophageal cancer cells: involvement of the p38MAPK signalling pathway. Nat Chem Biol 89 564 PMID: 12888831

Anderson et al (2011) Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR). Toxicol Lett 202 148 PMID: 21315811


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Reviews for PK 11195

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A peripheral benzodiazepine receptor (PBR) agonist..
By Anonymous on 05/02/2018
Assay Type: In Vitro
Species: Human

It is a peripheral benzodiazepine receptor (PBR) agonist. It is effective in inhibiting LPS-induced pro-inflammatory cytokines such as IL-1beta and TNF-alpha in microglia culture.


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