Catalog Number: 2764
Chemical Name: N-(Piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide
Biological Activity
Highly selective CB2 receptor agonist; Ki values are 0.037 and 363 nM for CB2 and CB1 receptors respectively. Increases P-ERK1/2 expression in HL-60 cells in vitro. More recently shown to be CB2 receptor inverse agonist/antagonist in cAMP, GTPγS and β-arrestin recruitment assays.
Technical Data
  • M.Wt:
    441.35
  • Formula:
    C23H22Cl2N4O
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    511532-96-0
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.
Background References
  1. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxam
    Murineddu et al.
    J.Med.Chem., 2006;49:7502
  2. The cannabinoid receptor 2 is critical for the host response to sepsis.
    Tschop et al.
    J.Immunol., 2009;183:499
  3. Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
    Soethoudt et al.
    Nat.Commun., 2017;
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GP 1a include:

5 Citations: Showing 1 - 5
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  1. Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
    Authors: Soethoudt Et al.
    Nat.Commun. 2017;
  2. CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion.
    Authors: Zhang Et al.
    Am J Physiol Regul Integr Comp Physiol 2015;8:3491
  3. Activation of cannabinoid receptor 2 inhibits experimental cystitis.
    Authors: Wang Et al.
    J Neuroimmune Pharmacol 2013;304:R846
  4. The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death.
    Authors: Robert Et al.
    Int J Clin Exp Pathol 2012;8:637
  5. Cannabinoid 2 (CB2) receptor involvement in the down-regulation but not up-regulation of serum IgE levels in immunized mice.
    Authors: Newton and Klein
    PLoS One 2012;7:591

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