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GP 1a

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Catalog No. T41231Cas No. 511532-96-0

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

GP 1a

GP 1a

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Purity: 99.96%
Catalog No. T41231Cas No. 511532-96-0
GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$51In StockIn Stock
5 mg$113In StockIn Stock
10 mg$178In StockIn Stock
25 mg$359In StockIn Stock
50 mg$533In StockIn Stock
100 mg$759In StockIn Stock
500 mg$1,530-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:99.96%
Appearance:Solid
Color:White
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COA HNMR LCMS

Product Introduction

GP 1a AI Summary
GP 1a exhibits a very high affinity for the CB2 receptor, with a Ki value of 0.037 nM in both spleen and brain tissues of CD1 mice, and a substantially lower affinity for the CB1 receptor (Ki = 363.0 nM). This results in a remarkable selectivity ratio (Ki) of 9810.0, reflecting a strong preference for CB2 over CB1 receptors. At a concentration of 10 nM, it significantly increases ERK1/2 phosphorylation activity in HL60 cells, indicating potent intrinsic activity at the CB2 receptor (83.0%). GP 1a also demonstrates inhibitory activities in various bioassays, including: - Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 22387.2 nM - Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) with a potency of 15848.9 nM - Fructose-1,6-bisphosphate Aldolase from Giardia Lamblia with a potency of 17740.7 nM - ROR gamma transcriptional activity with a potency of 35481.3 nM - GCN5L2 with a potency of 3981.1 nM - Binding or entry into cells for Lassa Virus and Marburg Virus with potencies of 35481.3 nM Moreover, GP 1a demonstrates antiviral activity. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells and VERO-6 cells at a concentration of 10 μM after 48 hours. It also shows 10.99% inhibition of SARS-CoV-2 3CL-Pro protease at 20 μM and exhibits minor inhibitory activity against human HDAC6. Overall, GP 1a’s highly selective interaction with the CB2 receptor, combined with its diverse bioactivity profile, including antiviral and enzyme inhibition effects, marks it as a compound of significant pharmacological potential..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.
Chemical Properties
Molecular Weight441.35
FormulaC23H22Cl2N4O
Cas No.511532-96-0
SmilesC(NN1CCCCC1)(=O)C=2C3=C(N(N2)C4=C(Cl)C=C(Cl)C=C4)C=5C(C3)=CC(C)=CC5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 90 mg/mL (203.92 mM), Sonication is recommended.
DMSO: 90 mg/mL (203.92 mM), Sonication is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.2658 mL11.3289 mL22.6578 mL113.2888 mL
5 mM0.4532 mL2.2658 mL4.5316 mL22.6578 mL
10 mM0.2266 mL1.1329 mL2.2658 mL11.3289 mL
20 mM0.1133 mL0.5664 mL1.1329 mL5.6644 mL
50 mM0.0453 mL0.2266 mL0.4532 mL2.2658 mL
100 mM0.0227 mL0.1133 mL0.2266 mL1.1329 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

PERKGP 1aCB2CannabinoidReceptorCannabinoid Receptor
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