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.
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- Formel: C21H21FN4O2
- Molecular Weight:380.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CB2R 54.6 nM (Ki) |
In Vitro
ISAM-CG557 (100 nM, 24 h) significantly reduces pro-inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6) and increases anti-inflammatory cytokines (IL-10, IL-4) in unstimulated and LPS (HY-D1056)-stimulated human THP-1 monocytes and Phorbol 12-myristate 13-acetate (PMA) (HY-18739)-differentiated macrophages[1].
ISAM-CG557 (100 nM) shows no toxicity to primary neurons isolated from fetal CD1 mouse brains, significantly restores cell viability reduced by LPS and IFN-γ, decreases ROS levels and caspase activity[1].
ISAM-CG557 (0.01 nM-1 μM, 48 h) concentration-dependently prevents neurite shortening induced by MAPT P301L and APP V717I plasmid transfection in Retinoic acid (HY-14649) and GLP-1 (HY-P3463)-differentiated SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 380.42
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Formel C21H21FN4O2
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SMILES
O=C([C@H]1N(C(C2=NN(CC3=CC=C(F)C=C3)C4=C2C=CC=C4)=O)CCCC1)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ISAM-CG557 Related Classifications
HY-175666 Related Classifications
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