Cannabinoid Receptor Agonist

ISAM-CG557 is a selective CB2R agonist, with a K_i 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.

MDA7 is the selective agonist for cannabinoid receptor 2 with EC₅₀ of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with K_i of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.

MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has K_i of 245 nM and 11 nM for CB1 and CB2. MN-25 has CB2 agonist activity and inhibits TNF-R release in human peripheral blood mononuclear cells in vitro with an IC₅₀ of 33 μM. MN-25 shows efficacy in a mouse acute inflammation model at oral doses up to 50 mg/kg^>[1].

TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB₂R agonist (EC₅₀: 51.2 nM) and a weak TRPM8 antagonist. TRPM8 antagonist 4 prodrug is a prodrug of TRPM8 antagonist 4 (HY-174825). TRPM8 antagonist 4 prodrug exhibits anti-inflammatory and analgesic activities and can be used in the research of inflammation-related pain disorders.

L-759656 is a selective cannabinoid CB2 receptor agonist, with the K_i of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin (HY-15371)-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC₅₀ of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.

VU6077967 is a selective cannabinoid receptor 2 (CB2) agonist with an EC₅₀ of 8.6 nM for rCB2. VU6077967 can be used for the research of neurological disease, suah as Alzheimer’s disease.

CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.

GW 833972A free base is a selective CB₂ receptor agonist with pEC₅₀ of the human CB₂ receptor for GW 833972A free base of 7.3, and its selectivity for the CB₂ receptor is approximately 1000 times higher than that for the CB₁ receptor. GW 833972A free base inhibits induced neuronal depolarization and suppresses coughing caused by citric acid in guinea pig models. GW 833972A free base can be used for the study of chronic cough.

CB2 receptor agonist 4 (Compound 8) is a highly selective cannabinoid receptor type 2 (CB2 Receptor) agonist with an EC₅₀ of 13.99 nM. CB2 receptor agonist 4 shows no significant activity against cannabinoid receptor type 1. CB2 receptor agonist 4 can be used for the research of pain and immune-related diseases.

CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC₅₀ and a K_i of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.

RD-pepcan-11 is a CB1 receptor agonist. RD-pepcan-11 increases the relative phosphorylation level of ERK1/2. RD-pepcan-11 mediates analgesic effects through interaction with CB1 receptors in a carrageenan-induced mouse inflammatory pain model. RD-pepcan-11 can be used in studies related to inflammatory pain.

15(S)-HETE Ethanolamide is a cannabinoid analog the CB1 receptor (K_i of 600 nM).

MDMB-FUBICA is a potent agonist of the cannabinoid receptors with psychoactive properties. MDMB-FUBICA can be used in the study of electronic cigarette.

CB2R agonist 2 (compound cis-17-para) is a CB2R agonist.

BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases.

(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with K_is of both 21 μM.

CB2 receptor agonist 6 (compound 70) is an agonist of CB2R, with EC₅₀ of 162 nM. The IC₅₀ values of CB2 receptor agonist 6 are 4.83 μM for CB1R and 0.88 μM for CB2R. CB2 receptor agonist 6 is a neuroprotective agent that can be used for the reseach of neurological disease.

CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The K_i values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC₅₀ value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

CB1-receptor agonist-1 is the racemic form of compound ‘1350 and is also a cannabinoid-1 receptor (CB1R) agonist.

CB2R/5-HT1AR agonist 1 (Compound 2o) is an orally active partial agonist of the CB₂ receptor (EC₅₀=479.6 nM). CB2R/5-HT1AR agonist 1 is a full agonist of 5-HT_1A receptor (EC₅₀=2.7 μM). CB2R/5-HT1AR agonist 1 exhibits anti-anxiety and anti-depressive effects. CB2R/5-HT1AR agonist 1 possesses favorable pharmacokinetic properties.