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PK 11195 (CAS 85532-75-8)

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Alternate Names:
1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Application:
PK 11195 is a peripheral benzodiazepine antagonist
CAS Number:
85532-75-8
Purity:
≥98%
Molecular Weight:
352.9
Molecular Formula:
C21H21ClN2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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PK 11195 is a peripheral benzodiazepine receptor (PBR) antagonist. The compound has been shown to help elicit the δPsim disruption and induce apoptosis. Furthermore, studies report that the apoptotic inhibition of activity of Bcl-2 is blocked by PK 1195 through its affect on the mitochondia. PK 11195 is also an activator of CAR.


PK 11195 (CAS 85532-75-8) References

  1. The pharmacodynamics of PK 11195 in diazepam-dependent male and female rats.  |  Sloan, JW., et al. 2000. Pharmacol Biochem Behav. 66: 751-64. PMID: 10973513
  2. Pharmacokinetics and effects on exercise heart rate of PK 11195 (52028 RP), an antagonist of peripheral benzodiazepine receptors, in healthy volunteers.  |  Ferry, A., et al. 1989. Fundam Clin Pharmacol. 3: 383-92. PMID: 2553568
  3. Differential binding properties of the peripheral-type benzodiazepine ligands [3H]PK 11195 and [3H]Ro 5-4864 in trout and mouse brain membranes.  |  Eshleman, AJ. and Murray, TF. 1989. J Neurochem. 53: 494-502. PMID: 2746235
  4. PK 11195, an antagonist of peripheral benzodiazepine receptors, reduces ventricular arrhythmias during myocardial ischemia and reperfusion in the dog.  |  Mestre, M., et al. 1985. Eur J Pharmacol. 112: 257-60. PMID: 2992998
  5. The Protective Effect of PK-11195 on Cognitive Impairment in Rats Survived of Polymicrobial Sepsis.  |  Dominguini, D., et al. 2021. Mol Neurobiol. 58: 2724-2733. PMID: 33495933
  6. The Effect of the Classical TSPO Ligand PK 11195 on In Vitro Cobalt Chloride Model of Hypoxia-like Condition in Lung and Brain Cell Lines.  |  Amara, R., et al. 2022. Biomolecules. 12: PMID: 36291606
  7. Differentiation between two ligands for peripheral benzodiazepine binding sites, [3H]RO5-4864 and [3H]PK 11195, by thermodynamic studies.  |  Le Fur, G., et al. 1983. Life Sci. 33: 449-57. PMID: 6308375
  8. PK 11195 aggravates 3,5-diethoxycarbonyl-1,4-dihydrocollidine-induced hepatic porphyria in rats.  |  Fonia, O., et al. 1996. Hepatology. 24: 697-701. PMID: 8781345
  9. PK 11195 antagonizes the positive inotropic response of the isolated rat heart to diazepam but not the negative inotropic response.  |  Leeuwin, RS., et al. 1996. Eur J Pharmacol. 299: 149-52. PMID: 8901017
  10. PK11195, a ligand of the mitochondrial benzodiazepine receptor, facilitates the induction of apoptosis and reverses Bcl-2-mediated cytoprotection.  |  Hirsch, T., et al. 1998. Exp Cell Res. 241: 426-34. PMID: 9637784

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PK 11195, 10 mg

sc-203199
10 mg
$88.00

PK 11195, 50 mg

sc-203199A
50 mg
$321.00