CB2R agonist-8
CB2R agonist-8 is a dual CB2R (Ki = 91.8 nM) agonist and FAAH (IC50 = 3.4 μM) inhibitor. CB2R agonist-8 signals through biased cAMP inhibition and β-arrestin recruitment, and reduces pro-inflammatory cytokine (TNF-α, IFN-γ, IL-1β, IL-6) production while increasing anti-inflammatory cytokine (IL-10 and IL-4) production in monocytes and macrophages. CB2R agonist-8 reduces reactive oxygen species (ROS) production in activated microglia. CB2R agonist-8 can be used for research on neuroinflammation and neurodegenerative diseases.
For research use only. We do not sell to patients.
- Formula: C32H37NO2
- Molecular Weight:467.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
hCB2-R 91.8 nM (Ki) |
hFAAH 3.4 μM (IC50) |
TNF-α |
IL-10 |
IL-6 |
IL-4 |
IL-1β |
In Vitro
CB2R agonist-8 (10 min) inhibits recombinant human FAAH with an IC50 of 3.4 μM[1].
CB2R agonist-8 (0.01 nM-10 μM; 90 min) is a unbiased CB2R agonist that induces cAMP inhibition with a pEC50 of 5.88 and β-arrestin-2 recruitment with a pEC50 of 5.35 in HEK293T CB2R-SmBiT/LgBiT-β-arrestin-2 cells[1].
CB2R agonist-8 (100 μM; 30 min) does not affect Calcein-AM transport in the P-glycoprotein (P-gp)-overexpressing MDCK-MDR1 cell line, i.e., it is not pumped out by P-gp[1].
CB2R agonist-8 (100 μM; 120 min) exhibits high bidirectional apparent permeability in the Caco-2 cell monolayer barrier model (Papp BA = 2307 nm/s; AB = 655 nm/s; BA/AB = 3.5), predicting good blood-brain barrier (BBB) penetration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 monocytes and PMA-differentiated THP-1 macrophages
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Concentration:1 μM and 5 μM
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Incubation Time:co-incubated for 24 hours during LPS stimulation
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Result:Significantly reduced the release of pro-inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6) and elevated the levels of anti-inflammatory cytokines (IL-10, IL-4).
Chemical Information
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Molecular Weight 467.64
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Formula C32H37NO2
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SMILES
CCCCCOC1=CC=C(C(C=C2)=CC3=C2C=CC=C3)C=C1C(NC4(C[C@H](C5)C6)C[C@@H]5C[C@@H]6C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CB2R agonist-8 Related Classifications
HY-190858 Related Classifications
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Keywords
- CB2R agonist-8
- Cannabinoid Receptor
- FAAH
- Reactive Oxygen Species (ROS)
- Arrestin
- Interleukin Related
- TNF Receptor
- Fatty acid amide hydrolase
- IL
- Tumor Necrosis Factor Receptor
- TNFR
- CB2R
- anandamide
- anti-inflammatory cytokine
- cAMP
- microglia
- neuroinflammation
- pro-inflammatory cytokine
- reactive oxygen species
- β-arrestin
- Inhibitor
- inhibitor
- inhibit