CB2R antagonist 3

• CAT Number: I042053
• Molecular Formula: C27H42N2O
• Molecular Weight: 410.64
• Purity: ≥95%
• Synonyms: N-(1-adamantyl)-5-pentyl-2-(pentylamino)benzamide
• InChI: InChI=1S/C27H42N2O/c1-3-5-7-9-20-10-11-25(28-12-8-6-4-2)24(16-20)26(30)29-27-17-21-13-22(18-27)15-23(14-21)19-27/h10-11,16,21-23,28H,3-9,12-15,17-19H2,1-2H3,(H,29,30)
• InChIKey: IWSAHCNAMZYEBW-UHFFFAOYSA-N
• SMILES: CCCCCC1=CC(=C(C=C1)NCCCCC)C(=O)NC23CC4CC(C2)CC(C4)C3

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 combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines[1].
CB2R antagonist 3 (compound 10a) (1 and 10 µM; 24 h) significantly reduces the TNF-α, IFN-γ, IL-1β, IL-6 pro-inflammatory cytokines expression and increases the IL-10 anti-inflammatory cytokines expression in monocytes and macrophages when combined with activator CB65 under the presence of lipopolysaccharide[1].

Reference

[1]. Graziano G, et al. N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R). Eur J Med Chem. 2023 Feb 15;248:115109.
 [Content Brief]