PK 11195

Pricing Availability Delivery Time Qty
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 (2)
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

PK 11195 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.64 50
ethanol 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.83 mL 14.17 mL 28.34 mL
5 mM 0.57 mL 2.83 mL 5.67 mL
10 mM 0.28 mL 1.42 mL 2.83 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for PK 11195, please let us know.

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View all Translocator Protein Ligands

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

2 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


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