AdipoGen Life Sciences

PK 11195

CHF 75.00
In stock
AG-CR1-0008-M01010 mgCHF 75.00
AG-CR1-0008-M05050 mgCHF 300.00
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Product Details
Synonyms 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Product Type Chemical
Properties
Formula

C21H21ClN2O

MW 352.9
CAS 85532-75-8
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in 100% ethanol, methanol, DMSO or dichloromethane; insoluble in water.
Identity Determined by 1H-NMR.
InChi Key RAVIZVQZGXBOQO-UHFFFAOYSA-N
Smiles CCC(C)N(C)C(=O)C1=CC2=C(C=CC=C2)C(=N1)C1=CC=CC=C1Cl
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage +4°C
Use/Stability Stable for at least 2 years after receipt when stored at +4°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Description
  • Selective peripheral benzodiazepine antagonist [1, 2].
  • Apoptosis enhancer [3, 5, 8].
  • Glucose-induced insulin secretion inhibitor [4].
  • Induces mitochondria cytochrome c release [6].
  • Anticancer compound [7].
  • Antiproliferative [9].
  • Pharmacological tool in autophagy [10].
Product References
  1. Differentiation between two ligands for peripheral benzodiazepine binding sites, [3H]RO5-4864 and [3H]PK 11195, by thermodynamic studies: G. Le Fur et al.; Life Sci. 33, 449 (1983) 
  2. Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination: A. Doble et al.; Eur. J. Pharmacol. 119, 153 (1985) 
  3. PK11195, a ligand of the mitochondrial benzodiazepine receptor, facilitates the induction of apoptosis and reverses Bcl-2-mediated cytoprotection: T. Hirsch et al.; Exp. Cell. Res. 241, 426 (1998) 
  4. Inhibition of glucose-induced insulin secretion by a peripheral-type benzodiazepine receptor ligand (PK11195): D. Pujalte, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 362, 46 (2000)
  5. PK11195 potently sensitizes to apoptosis induction independently from the peripheral benzodiazepin receptor: R.A. Gonzalez-Polo, et al.; Oncogene 24, 7503 (2005) 
  6. Peripheral benzodiazepine receptor ligand, PK11195 induces mitochondria cytochrome c release and dissipation of mitochondria potential via induction of mitochondria permeability transition: J. Li, et al.; Eur. J. Pharmacol. 560, 117 (2007) 
  7. The potential anticancer agent PK11195 induces apoptosis irrespective of p53 and ATM status in chronic lymphocytic leukemia cells: A.F. Santidrian et al.; Haematologica 92, 1631 (2007) 
  8. Modulation of intracellular Ca2+ signalling in HeLa cells by the apoptotic cell death enhancer PK11195: M. Campanella et al.; Biochem. Pharmacol. 76, 1628 (2008) 
  9. Antiproliferative effect of peripheral benzodiazepine receptor antagonist PK11195 in rat mammary tumor cells: S. Mukhopadhyay et al.; Mol. Cell. Biochem. 340, 203 (2010) 
  10. Ca2+-dependent autophagy is enhanced by the pharmacological agent PK11195: Pharmacological tools in autophagy: A. Gastaldello, et al.; Autophagy 6 607 (2010) 
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