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Cannabinoid Receptor Inhibitors/Activators | Agonists | Antagonists | Modulators

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Cannabinoid Receptor Products

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  • Cannabinoid Receptor Antagonists (7)
  • Cannabinoid Receptor Agonists (8)
  • Cannabinoid Receptor Modulators (2)
  • New Cannabinoid Receptor Products
Cat.No. Product Name Information Product Use Citations Product Validations
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, and this compound exhibits 82-fold selectivity over CB1 receptor.
Cell Rep, 2025, 44(4):115559
CNS Neurosci Ther, 2025, 31(8):e70591
Redox Rep, 2024, 29(1):2420572
Verified customer review of AM1241
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Biol Pharm Bull, 2025, 48(6):769-781
Pharmacol Res, 2023, 194:106864
Physiol Rep, 2023, 11(1):e15565
Verified customer review of AM251
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. It is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Biol Pharm Bull, 2025, 48(6):769-781
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Nat Commun, 2020, 11(1):71
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
S2854 BML-190 BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Int J Mol Sci, 2020, 21(7)
University of Alberta, 2014, Yahya Muhammad Fiteih
Verified customer review of BML-190
S8033 6-Iodopravadoline (AM630) AM630 (6-Iodopravadoline) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Brain Behav Immun, 2023, 110:60-79
Pharmacol Res, 2023, 194:106864
S2778 GW842166X GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Nat Commun, 2020, 11(1):71
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
Biochem Pharmacol, 2024, 224:116190
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
S8017 WIN 55, 212-2 mesylate WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.
Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
E4945 Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).
E0458 RTICBM-189 RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.
E1841 Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585 N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells.
E4858 Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.
S9048 (+)-Gallocatechin (+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. This compound displays analgesic properties.
S9413 Yangonin Yangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors.
S8694 CID16020046 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Pharmacol Res, 2024, 203:107176
A2574 Nimacimab (Anti-CB1 / CNR1) Nimacimab (Anti-CB1/CNR1) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases. MW:145.5 KD.
A2575 Anti-CB1 / CNR1 Anti-CB1 / CNR1 (GFB-024) is a recombinant humanised monoclonal antinody that is used for targeting of CB1 receptor. MW:145.5 KD.
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.
E4945 Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).
A2574 Nimacimab (Anti-CB1 / CNR1) Nimacimab (Anti-CB1/CNR1) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases. MW:145.5 KD.
A2575 Anti-CB1 / CNR1 Anti-CB1 / CNR1 (GFB-024) is a recombinant humanised monoclonal antinody that is used for targeting of CB1 receptor. MW:145.5 KD.
S9413 Yangonin Yangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors.
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Biol Pharm Bull, 2025, 48(6):769-781
Pharmacol Res, 2023, 194:106864
Physiol Rep, 2023, 11(1):e15565
 Verified customer review of AM251
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. It is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Biol Pharm Bull, 2025, 48(6):769-781
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Nat Commun, 2020, 11(1):71
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
S8033 6-Iodopravadoline (AM630) AM630 (6-Iodopravadoline) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Brain Behav Immun, 2023, 110:60-79
Pharmacol Res, 2023, 194:106864
E4858 Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.
S8694 CID16020046 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Pharmacol Res, 2024, 203:107176
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, and this compound exhibits 82-fold selectivity over CB1 receptor.
Cell Rep, 2025, 44(4):115559
CNS Neurosci Ther, 2025, 31(8):e70591
Redox Rep, 2024, 29(1):2420572
 Verified customer review of AM1241
S2854 BML-190 BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Int J Mol Sci, 2020, 21(7)
University of Alberta, 2014, Yahya Muhammad Fiteih
Verified customer review of BML-190
S2778 GW842166X GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Nat Commun, 2020, 11(1):71
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
Biochem Pharmacol, 2024, 224:116190
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
S8017 WIN 55, 212-2 mesylate WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.
Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
E1841 Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585 N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells.
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. This compound displays analgesic properties.
E0458 RTICBM-189 RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.
S9048 (+)-Gallocatechin (+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.

Signaling Pathway Map