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GP 1a

Cat. No. 2764 6 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: CB2 receptor inverse agonist
Chemical Name: N-(Piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations (6)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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

M. Wt 441.35
Formula C23H22Cl2N4O
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 511532-96-0
PubChem ID 10252734
InChI Key FNOMTMVRTBHRET-UHFFFAOYSA-N
Smiles CC1=CC2=C(C=C1)C1=C(C2)C(=NN1C1=CC=C(Cl)C=C1Cl)C(=O)NN1CCCCC1

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
Solubility
DMSO 44.13 100
ethanol 44.13 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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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6 Citations for GP 1a

Citations are publications that use Tocris products. Selected citations for GP 1a include:

Wang et al (2013) Activation of cannabinoid receptor 2 inhibits experimental cystitis. J Neuroimmune Pharmacol 304 R846 PMID: 23515618

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

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

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

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

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

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Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.