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Biological Activity for GP 1a
GP 1a is a 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.
Technical Data for GP 1a
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GP 1a
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GP 1a
The following data is based on the product molecular weight 441.35. Batch specific molecular weights may vary from batch to batch due to the degree 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 for GP 1a
References are publications that support the biological activity of the product.
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, GP 1a supplier, selective, CB2, receptor, agonists, cannabinoid, receptors, GP1a, cb2r, Receptors, 2764, Tocris Bioscience
6 Citations for GP 1a
Citations are publications that use Tocris products. Selected citations for GP 1a include:
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
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
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
Sheng et al (2019) Antiallodynic Effects of Cannabinoid Receptor 2 (CB2R) Agonists on Retrovirus Infection-Induced Neuropathic Pain. Pain Res Manag 2019 1260353 PMID: 31354896
Soethoudt et al (2017) Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. PMID: 28045021
Do you know of a great paper that uses GP 1a from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.