GP 1a

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Cat.No. 2764 - GP 1a | C23H22Cl2N4O | CAS No. 511532-96-0
Description: Highly selective CB2 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 (4)
Literature

Biological Activity

Highly selective CB2 receptor agonist; Ki values are 0.037 and 363 nM for CB2 and CB1 receptors respectively. Increases P-ERK1/2 expression in HL-60 cells in vitro.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.13 100
ethanol 44.13 100

Preparing Stock Solutions

The following data is based on the product molecular weight 441.35. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: GP 1a, supplier, selective, CB2, receptor, agonists, cannabinoid, receptors, GP1a, cb2r, CB2, Receptors, Tocris Bioscience

4 Citations for GP 1a

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

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

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

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


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

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Pathways for GP 1a

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