ISAM-CG557

ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK) . ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders[1].

Product Specifications

UNSPSC

12352100

Target

Arrestin; Cannabinoid Receptor; Caspase; p38 MAPK; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Field of Research

Inflammation/Immunology; Neurological Disease

Smiles

O=C([C@H]1N(C(C2=NN(CC3=CC=C(F)C=C3)C4=C2C=CC=C4)=O)CCCC1)N

Molecular Formula

C21H21FN4O2

Molecular Weight

380.42

References & Citations

[1]Gioé-Gallo C, et al. Conformational Restriction of Designer Drugs Reveals Subtype-Selective and Biased CB2 Agonists with Neuroprotective Effects. J Med Chem. 2025 Aug 28;68 (16) :17103-17129.