2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cannabinoid Receptor
  5. CB1 Isoform
  6. CB1 Agonist

CB1 Agonist

CB1 Agonists (41):

Cat. No. Product Name Effect Purity
  • HY-10863
    Anandamide
    		Agonist ≥99.0%
    Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.
  • HY-168997
    CB1R agonist 1
    		Agonist
    CB1R agonist 1 (Compound '1350') is a potent full agonist of the cannabinoid-1 receptor (CB1R), with a Ki value of 0.95 nM. CB1R agonist 1 exhibits significant pain-reducing effects in multiple pain models, including acute heat pain, inflammatory pain, and neuropathic pain.
  • 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.
  • HY-100197
    Synaptamide
    		Agonist 99.30%
    Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .
  • HY-W005629
    Leelamine
    		Agonist 98.36%
    Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells.
  • HY-110036
    GW-405833
    		Agonist 99.12%
    GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain.
  • HY-110028
    Leelamine hydrochloride
    		Agonist 99.06%
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
  • HY-116637
    Tetrahydromagnolol
    		Agonist 99.79%
    Tetrahydromagnolol (Magnolignan), the main metabolite of Magnolol, is a potent and selective cannabinoidCB2 receptor agonist (EC50 =170 nM) and GPR55 antagonist. The Ki of Tetrahydromagnolol for CB2 is 416 nM, 20-fold higher than for the CB1 receptor. Magnolol shows antifungal, anti-inflammatory and analgesic effects.
  • HY-100488
    Bay 59-3074
    		Agonist 98.60%
    Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
  • HY-150029
    CB1/2 agonist 3
    		Agonist 99.83%
    CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively.
  • HY-147512
    CB1/2 agonist 1
    		Agonist 99.20%
    CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.
  • HY-119104
    AZD1940
    		Agonist 99.58%
    AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
  • HY-113689
    GAT211
    		Agonist 99.98%
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.
  • HY-101389
    (R)-Methanandamide
    		Agonist
    (R)-Methanandamide (AM-356), an analog of the endocannabinoid ligand Anandamide, is a potent CB1 agonist with a Ki of 20 nM. (R)-Methanandamide also activates vanilloid (TRPV1) receptors.
  • HY-W013788
    2-Palmitoylglycerol
    		Agonist ≥99.0%
    2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.
  • HY-P1397A
    RVD-Hpα TFA
    		Agonist 99.32%
    RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-110014
    Noladin ether
    		Agonist ≥98.0%
    Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.
  • HY-152254
    CB2R/FAAH modulator-3
    		Agonist 99.71%
    CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.
  • HY-110040
    L759633
    		Agonist ≥99.0%
    L759633 is a potent and selective agonist of cannabinoid receptor (CB2) receptor, with Kis of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production.
  • HY-110018
    N-Arachidonyldopamine
    		Agonist 98.36%
    N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM.