2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

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Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Cannabinoid Receptor Isoform Specific Products:

Cannabinoid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W705168
    Yangonin-d3
    Yangonin-d3 is the deuterium labeled Yangonin (HY-N0919). Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin-d<sub>3</sub>
  • HY-178448
    EGFR-IN-178
    		Activator
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-116380
    CB2 receptor antagonist 5
    CB2 receptor antagonist 5 (compound 4A) is a ligand of CB2 receptor with antagonist effect.
    CB2 receptor antagonist 5
  • HY-14160
    CB2 receptor agonist 7
    		Agonist
    CB2 receptor agonist 7 (Compound 5B) is a cannabinoid 2 (CB2) receptor agonist with blood-brain barrier permeability.
    CB2 receptor agonist 7
  • HY-W777527
    AM404-d4
    AM404-d4 is the deuterium labeled AM404 (HY-101388). AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Neuroprotective Effect.
    AM404-d<sub>4</sub>
  • HY-164913
    PSB-SB-1203
    		Modulator
    PSB-SB-1203 (Compound 25b) is a dual CB1/CB2 ligand that blocks CB1 but activates CB2 receptors (CB1 Ki 0.244 μM; CB2 Ki 0.210 μM, EC50 0.054 μM). PSB-SB-1203 is promising for research of obesity and cancers.
    PSB-SB-1203
  • HY-100778
    SMM-189
    		Agonist
    SMM-189 is  a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research.
    SMM-189
  • HY-175666
    ISAM-CG557
    		Agonist
    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.
    ISAM-CG557
  • HY-155967
    CB1R/AMPK modulator 1
    		Antagonist
    CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity.
    CB1R/AMPK modulator 1
  • HY-173083
    MDA7
    		Agonist
    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 Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.
    MDA7
  • HY-118656
    Cannabicitran
    		Ligand
    Cannabicitran is a cannabinoid. Cannabicitran can decrease intraocular pressure in rabbits.
    Cannabicitran
  • HY-169820
    CE-178253 benzenesulfonate
    		Antagonist
    CE-178253 benzenesulfonate is a CB1 antagonist with central nervous system activity.
    CE-178253 benzenesulfonate
  • HY-124954
    MN-25
    		Agonist
    MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has Ki 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].
    MN-25
  • HY-174846
    TRPM8 antagonist 4 prodrug
    		Agonist
    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.
    TRPM8 antagonist 4 prodrug
  • HY-110041
    L-759656
    		Agonist
    L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki 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.
    L-759656
  • HY-W008364S1
    Olivetol-d9
    Olivetol-d9 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activities.
    Olivetol-d<sub>9</sub>
  • HY-164817
    CB1/2 receptor-1
    		Agonist
    CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.
    CB1/2 receptor-1
  • HY-180365
    GW 833972A free base
    		Agonist
    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.
    GW 833972A free base
  • HY-155741
    CB2 PET Radioligand 1
    CB2 PET Radioligand 1 (compound [18F]9) is a PET Radioligand targeting to hCB2 (Ki=7.7 nM). CB2 PET Radioligand 1 is prepared with Cu-mediated 18F-fluorination. CB2 PET Radioligand 1 shows high brain uptake in a murine model of neuroinflammation.
    CB2 PET Radioligand 1
  • HY-153693
    CB2 receptor agonist 4
    		Agonist
    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.
    CB2 receptor agonist 4
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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