cb2r-in-1

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

PROTACCB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that employs the ubiquitin-proteasome system (UPS) to facilitate CB1R degradation, showing a DC50 of 3.37 μM in MCF-7 cells while exhibiting no effect on CB2R. It reduces CB1R-associated downstream signaling pathways (p-AKT, p-ERK, BCL2, and MCM5), thus inhibiting breast cancer cell proliferation and inducing apoptosis. PROTACCB1R Degrader-1 is applicable for breast cancer-related research.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

CB2R-IN-3 is a selective antagonist of cannabinoid type 2 receptor (CB2R) . CB2R-IN-3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R-IN-3 can be combined with CB65 , the activator of CB2R. CB2R-IN-3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines [1] .

CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].