| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
CB2 cannabinoid receptor. GP 2A is a selective CB2 receptor agonist with Ki values of 7.6 nM for CB2 and 900 nM for CB1 receptors, demonstrating approximately 118-fold selectivity for CB2 over CB1. This high selectivity is critical for studying CB2-specific functions without the confounding psychoactive effects associated with CB1 receptor activation.
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| ln Vitro |
CB2 receptor agonist 3 (compound 2a) has also been demonstrated to be an agonist in an in vitro model using HL-60 human promyelocytic leukemia cells [1].
GP 2A binds to the CB2 receptor with a Ki of 7.6 nM and to the CB1 receptor with a Ki of 900 nM, demonstrating ~118-fold selectivity for CB2. The compound significantly increases P-ERK1/2 expression in HL-60 cells in vitro. In functional assays, GP 2A activates CB2-mediated signaling pathways, including the MAPK/ERK cascade. The compound shows modest agonism at CB1 receptors at higher concentrations. The tricyclic pyrazole scaffold of GP 2A provides a distinct pharmacophore for CB2 receptor activation. |
| ln Vivo |
In vivo efficacy of GP 2A has not been extensively characterized in publicly available literature. As a selective CB2 agonist, it would be expected to show anti-inflammatory and immunomodulatory effects in animal models of inflammation, neuropathic pain, and autoimmune diseases based on the established pharmacology of CB2 receptor activation. CB2 receptor agonists are known to modulate immune cell function, reduce pro-inflammatory cytokine production, and attenuate pain responses without the psychoactive effects associated with CB1 activation. Specific animal model data and dosing regimens are limited in publicly available sources.
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| Enzyme Assay |
CB2 receptor binding affinity is assessed using in vitro radioligand binding assays with membrane preparations from cells expressing recombinant human CB2 or CB1 receptors. Competitive binding with [3H]CP-55,940 or other selective radioligands is measured. Ki values are calculated from displacement curves using nonlinear regression analysis (e.g., Cheng-Prusoff equation). Agonist activity is evaluated using cAMP inhibition assays (measuring the decrease in forskolin-stimulated cAMP accumulation) or β-arrestin recruitment assays (e.g., PathHunter or Tango assays). Selectivity is confirmed by parallel testing in CB1-expressing cells.
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| Cell Assay |
Cellular activity is evaluated in HL-60 cells (human promyelocytic leukemia cells) or other immune cells expressing CB2 receptors. Cells are treated with GP 2A at various concentrations (typically 0.001-100 μM) for appropriate time periods (e.g., 5-60 minutes for signaling assays, 24-72 hours for functional responses). P-ERK1/2 expression is measured by Western blot using phospho-specific antibodies (pERK1/2) and total ERK1/2 as loading control. cAMP levels are measured by ELISA or HTRF-based assays. Cell viability and proliferation may be assessed by MTT or CellTiter-Glo assays. Calcium mobilization may be measured using fluorescent calcium indicators (e.g., Fluo-4 AM) in cells expressing CB2 receptors.
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| Animal Protocol |
In vivo studies for GP 2A are limited. Potential studies could be conducted in rodent models of inflammation (e.g., carrageenan-induced paw edema, CFA-induced arthritis), neuropathic pain (e.g., spared nerve injury, streptozotocin-induced diabetic neuropathy), or autoimmune diseases (e.g., EAE, colitis). GP 2A would be administered orally, intraperitoneally, or subcutaneously at doses determined from preliminary pharmacokinetic and tolerability studies. Inflammatory markers (cytokine levels, immune cell infiltration), pain responses (von Frey filaments, hot plate, tail flick), and disease severity scores would be assessed. Pharmacodynamic markers include CB2 receptor occupancy and downstream signaling activation in target tissues. Specific protocols are not detailed in publicly available literature.
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| ADME/Pharmacokinetics |
GP 2A has a molecular formula of C24H23Cl2N3O and a molecular weight of 440.36 g/mol. Purity is typically ≥99% by HPLC. CAS Number: 919077-81-9. Storage: store at room temperature or -20°C for long-term stability. The compound is soluble in DMSO. Log Po/w and other physicochemical properties are available from the literature. Detailed pharmacokinetic parameters including half-life, oral bioavailability, volume of distribution, and plasma protein binding are not extensively characterized in publicly available literature.
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| Toxicity/Toxicokinetics |
Safety data for GP 2A indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity (LD50), organ toxicity, genotoxicity, and reproductive toxicity are not extensively published. As a CB2 agonist, it may have immune-modulating effects that could impact immune function. The compound should be handled with standard laboratory safety precautions, including the use of personal protective equipment (gloves, lab coat, safety goggles) and adequate ventilation. Avoid inhalation, ingestion, and skin contact. The compound is for research use only and not for human or veterinary therapeutic applications. Consult the material safety data sheet (MSDS) for detailed safety information.
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| References | |
| Additional Infomation |
N-Cyclohexyl-1-(2,4-dichlorophenyl)-6-methyl-4H-indeno[1,2-c]pyrazole-3-carboxamide is a member of the pyrazole class of compounds and cyclic compounds.
GP 2A is a research tool compound for studying CB2 receptor biology and cannabinoid signaling. It is not approved for clinical use. The compound has been investigated for its potential in inflammation and pain research. Reference: Murineddu et al (2006) J. Med. Chem. 49 7502, which describes the synthesis and pharmacological characterization of GP 2A as a selective CB2 receptor agonist. The compound's high selectivity for CB2 over CB1 (~118-fold) makes it a valuable tool for dissecting CB2-specific functions in immune modulation, pain pathways, and inflammatory diseases without the confounding psychoactive effects associated with CB1 activation. |
| Molecular Formula |
C24H23CL2N3O
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|---|---|
| Molecular Weight |
440.36
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| Exact Mass |
439.121
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| CAS # |
919077-81-9
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| PubChem CID |
16094766
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
632.9±55.0 °C at 760 mmHg
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| Flash Point |
336.6±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.700
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| LogP |
6.58
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SPEFJYZGXZENAF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23Cl2N3O/c1-14-7-9-18-15(11-14)12-19-22(24(30)27-17-5-3-2-4-6-17)28-29(23(18)19)21-10-8-16(25)13-20(21)26/h7-11,13,17H,2-6,12H2,1H3,(H,27,30)
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| Chemical Name |
N-cyclohexyl-1-(2,4-dichlorophenyl)-6-methyl-4H-indeno[1,2-c]pyrazole-3-carboxamide
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| Synonyms |
GP2A GP-2A GP 2A
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~28.39 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2709 mL | 11.3543 mL | 22.7087 mL | |
| 5 mM | 0.4542 mL | 2.2709 mL | 4.5417 mL | |
| 10 mM | 0.2271 mL | 1.1354 mL | 2.2709 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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