CB2 receptor inverse agonist (pEC50 = 7.1), shown in cAMP, GTPγS and β-arrestin recruitment assays. Demonstrates approximately 30-fold selectivity for CB2 receptors over CB1 receptors. Increases P-ERK1/2 expression in HL-60 cells in vitro.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 441.35. 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||2.27 mL||11.33 mL||22.66 mL|
|5 mM||0.45 mL||2.27 mL||4.53 mL|
|10 mM||0.23 mL||1.13 mL||2.27 mL|
|50 mM||0.05 mL||0.23 mL||0.45 mL|
References are publications that support the products' biological activity.
Murineddu et al (2006) 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 J.Med.Chem. 49 7502 PMID: 17149879
Tschop et al (2009) The cannabinoid receptor 2 is critical for the host response to sepsis. J.Immunol. 183 499 PMID: 19525393
Soethoudt et al (2017) Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. 8 13958 PMID: 28045021
If you know of a relevant reference for GP 1a, please let us know.
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Keywords: GP 1a, supplier, selective, CB2, receptor, agonists, cannabinoid, receptors, GP1a, cb2r, CB2, Receptors, CB2, Receptors, Tocris Bioscience
5 Citations for GP 1a
Citations are publications that use Tocris products. Selected citations for GP 1a include:
Robert et al (2012) The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death. Int J Clin Exp Pathol 8 637 PMID: 22498477
Soethoudt et al (2017) Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. PMID: 28045021
Zhang et al (2015) CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion. Am J Physiol Regul Integr Comp Physiol 8 3491 PMID: 26097533
Newton and Klein (2012) Cannabinoid 2 (CB2) receptor involvement in the down-regulation but not up-regulation of serum IgE levels in immunized mice. PLoS One 7 591 PMID: 22552780
Wang et al (2013) Activation of cannabinoid receptor 2 inhibits experimental cystitis. J Neuroimmune Pharmacol 304 R846 PMID: 23515618
Do you know of a great paper that uses GP 1a from Tocris? If so please let us know.
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Literature in this Area
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