GP 1a

Pricing Availability   Qty

Save up to 40% on RUO Reagents with BIOSPRING24 (see 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: ≥99% (HPLC)
Citations (6)
Literature (1)

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
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
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

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.

View Related Products by Target

View Related Products by Product Action

View all CB2 Receptor Inverse Agonists

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:

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

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

Do you know of a great paper that uses GP 1a from Tocris? Please let us know.

Reviews for GP 1a

There are currently no reviews for this product. Be the first to review GP 1a and earn rewards!

Have you used GP 1a?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

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.

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.