CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be used in combination with CB65, an activator of CB2R. CB2R antagonist 3 effectively upregulates the expression of anti-inflammatory cytokines and downregulates the expression of pro-inflammatory cytokines.

Physicochemical Properties

Molecular Formula	C27H42N2O
Molecular Weight	410.64
Appearance	Solid powder
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	CB2R
ln Vitro	When CB2R antagonist 3 (compound 10a) (1 and 10 µM; 24 h) was combined with the activator CB65, it significantly reduced the expression of pro-inflammatory cytokines TNF-α, IFN-γ, IL-1β, and IL-6, and increased the expression of anti-inflammatory cytokine IL-10 in the presence of lipopolysaccharide [1].
References	[1]. N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R). Eur J Med Chem. 2023 Feb 15;248:115109.

Solubility Data

Solubility (In Vitro)	DMSO : 100 mg/mL (243.52 mM; with sonication (<60°C))
Solubility (In Vivo)	Solubility in Formulation 1: 2.5 mg/mL (6.09 mM) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; sonication aided. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4352 mL	12.1761 mL	24.3522 mL
	5 mM	0.4870 mL	2.4352 mL	4.8704 mL
	10 mM	0.2435 mL	1.2176 mL	2.4352 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.