GP 1a

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

Citations (29)

COA / SDS

CB2 receptor inverse agonist

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Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

CB2 receptor inverse agonist

View all Cannabinoid R2/CB2 Inverse Agonists »

Product Description

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.

Product Specifications

Molecular Weight

441.35

Formula

C₂₃H₂₂Cl₂N₄O

Storage

Store at RT

Purity

≥98% (HPLC)

Chemical Name

N-(Piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide

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.

Solubility

	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 all 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

Calculators

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Background References

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