GP 1a

Tocris Bioscience, part of Bio-Techne | Catalog # 2764

COA / SDS

CB2 receptor inverse agonist

Key Product Details

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:	≥98% (HPLC)
Molecular Weight:	441.35

View Full Technical Details for GP 1a

Technical Data
Citations

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	≥98% (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 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.

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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Reconstitution Calculator

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References for GP 1a

References are publications that support the biological activity of the product.

Tschop The cannabinoid receptor 2 is critical for the host response to sepsis. J.Immunol. 2009 PMID: 19525393
Soethoudt Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity. Nat.Commun. 2017 PMID: 28045021
Murineddu 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. 2006 PMID: 17149879