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| Targets |
GP1a targets cannabinoid receptor 2 (CB2), a G protein-coupled receptor that is primarily expressed on immune cells, including B cells, natural killer cells, and macrophages. CB2 receptors are involved in the modulation of immune responses, inflammation, and pain. By acting as a potent agonist of CB2, GP1a activates CB2-mediated signaling pathways, including inhibition of adenylyl cyclase and activation of ERK1/2. Its approximately 30-fold selectivity for CB2 over CB1 makes it a valuable tool for studying CB2 biology and for developing CB2-targeted therapies.
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| ln Vitro |
In vitro, GP1a is a potent agonist of CB2 with an EC50 of 7.1 nM in cAMP, GTPγS, and β-arrestin recruitment assays. It shows approximately 30-fold selectivity for CB2 over CB1. In cell-based assays, GP1a increases P-ERK1/2 expression in HL-60 cells. Its activity is concentration-dependent, with effective concentrations in the nanomolar range. Its potent and selective CB2 agonism makes it a valuable tool for studying CB2 function, immune modulation, and inflammation.
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| ln Vivo |
In vivo, GP1a is beneficial for skin wound healing. It inhibits inflammation and fibrogenesis while promoting re-epithelialization. Administration of GP1a in animal models results in improved wound healing outcomes. Its ability to modulate CB2-mediated immune responses supports its potential for treating inflammatory and fibrotic conditions. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources.
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| Enzyme Assay |
The in vitro CB2 activation assay for GP1a typically uses cells expressing recombinant human CB2 (e.g., CHO cells) and measures cAMP accumulation, GTPγS binding, or β-arrestin recruitment. For cAMP assays, cells are treated with varying concentrations of the test compound (typically 0.01 nM to 10 µM) and forskolin, and cAMP levels are measured using a competitive ELISA or HTRF-based cAMP detection kit. For GTPγS binding assays, membranes from CB2-expressing cells are incubated with [³⁵S]-GTPγS and varying concentrations of the compound. EC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., known CB2 agonists) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, HL-60 cells or other CB2-expressing cells are treated with GP1a at concentrations ranging from 0.01 nM to 10 µM for 1-24 hours. ERK1/2 phosphorylation is assessed by Western blotting. Cell viability is assessed using MTT or CellTiter-Glo assays. For wound healing studies, cell migration is assessed using scratch assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo wound healing studies, rodent models of skin wound healing are used. GP1a is administered topically or intraperitoneally at doses ranging from 0.1 to 10 mg/kg. Wound healing is assessed by measuring wound closure area. Inflammation and fibrogenesis are assessed by histological analysis and measurement of inflammatory markers. Re-epithelialization is assessed by immunohistochemistry. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of GP1a have been partially characterized. The compound has a molecular weight of 441.35 and a molecular formula of C23H22Cl2N4O. Following topical or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including skin. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of GP1a are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
1-(2,4-dichlorophenyl)-6-methyl-N-(1-piperidinyl)-4H-indo[1,2-c]pyrazole-3-carboxamide is a pyrazole compound and a cyclic compound.
GP1a is a potent agonist of CB2 (EC50 = 7.1 nM) with approximately 30-fold selectivity over CB1. It increases P-ERK1/2 expression and is beneficial for skin wound healing. It inhibits inflammation and fibrogenesis while promoting re-epithelialization. It is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use. |
| Molecular Formula |
C23H22CL2N4O
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|---|---|
| Molecular Weight |
441.352982997894
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| Exact Mass |
440.117
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| CAS # |
511532-96-0
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| PubChem CID |
10252734
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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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| Index of Refraction |
1.711
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| LogP |
5.23
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)C3=C(C2)C(=NN3C4=C(C=C(C=C4)Cl)Cl)C(=O)NN5CCCCC5
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| InChi Key |
FNOMTMVRTBHRET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22Cl2N4O/c1-14-5-7-17-15(11-14)12-18-21(23(30)27-28-9-3-2-4-10-28)26-29(22(17)18)20-8-6-16(24)13-19(20)25/h5-8,11,13H,2-4,9-10,12H2,1H3,(H,27,30)
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| Chemical Name |
1-(2,4-dichlorophenyl)-6-methyl-N-piperidin-1-yl-4H-indeno[1,2-c]pyrazole-3-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~283.22 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 | 2.2658 mL | 11.3289 mL | 22.6578 mL | |
| 5 mM | 0.4532 mL | 2.2658 mL | 4.5316 mL | |
| 10 mM | 0.2266 mL | 1.1329 mL | 2.2658 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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