CB2
Cannabinoid receptor CB2 (CB2R) is a cannabinoid G protein-coupled receptor originally characterized as a peripheral receptor expressed in macrophages and immune tissues[1][2]. Mechanistically, CB2R couples through Gi/o proteins, inhibits adenylyl cyclase, and activates MAPK signaling, linking cannabinoid receptor signaling to immune-cell regulation[3]. In inflammatory biology, CB2R modulates immune-cell functions in cell systems and animal models, and CB2-deficient mice show exacerbated inflammatory phenotypes[2]. In neuroinflammation, CB2R activity is especially relevant in macrophage-lineage cells and CNS microglia, connecting peripheral immune regulation with central immune responses[4]. Compared with CB1, CB2 is distinguished by immune-enriched distribution, while CB1 is found predominantly in neuronal tissues and also couples to ion-channel signaling[5]. For experimental applications, CB2-selective agonists such as HU-308 bind CB2 efficiently, inhibit forskolin-stimulated cyclic AMP production in CB2-transfected cells, and support receptor-selective studies of inflammation and peripheral analgesia[6].- CB2R links cannabinoid receptor signaling with immune modulation, inflammation models, and neuroimmune research design[2][4]. - CB2 differs from CB1 mainly by immune distribution, not by complete separation of signaling pathways[5]. - HU-308 supports CB2-selective pharmacology studies in inflammation, peripheral analgesia, and cAMP assays[6].
References:
- [1]. Munro S, et al. Molecular characterization of a peripheral receptor for cannabinoids. Nature. 1993 Sep 2;365(6441):61-5. [Content Brief]
- [2]. Turcotte C, et al. The CB2 receptor and its role as a regulator of inflammation. Cell Mol Life Sci. 2016 Dec;73(23):4449-4470. [Content Brief]
- [3]. Howlett AC. Cannabinoid receptor signaling. Handb Exp Pharmacol. 2005;(168):53-79. [Content Brief]
- [4]. Cabral GA, et al. Emerging role of the cannabinoid receptor CB2 in immune regulation: therapeutic prospects for neuroinflammation. Expert Rev Mol Med. 2009 Jan 20;11:e3. [Content Brief]
- [5]. Howlett AC, et al. International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev. 2002 Jun;54(2):161-202. [Content Brief]
- [6]. Hanus L, et al. HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor. Proc Natl Acad Sci U S A. 1999 Dec 7;96(25):14228-33. [Content Brief]
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CB2 Related Products (82)
Related Products (82)
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CB2 receptor agonist 8
0 ImagesCat. No.: HY-168338CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87.
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Neuroprotective agent 15
0 ImagesCat. No.: HY-178943CAS No.: 2476614-40-9Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
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hBChE-IN-2
0 ImageshBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities.
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BAY 38-7271
0 ImagesCat. No.: HY-119744CAS No.: 212188-60-8BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
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CB2R-IN-1
0 ImagesCat. No.: HY-100328CAS No.: 1257555-79-5CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
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CB2R agonist 3
0 ImagesCat. No.: HY-149644CAS No.: 444331-43-5CB2R agonist 3 is an agonist of cannabinoid receptor 2 (CB2R), with EC50 of 0.37μM that plays an important role in immune system.
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SMM-189
0 ImagesCat. No.: HY-100778CAS No.: 1054451-07-8SMM-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.
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ISAM-CG557
0 ImagesCat. No.: HY-175666ISAM-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.
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MDA7
0 ImagesCat. No.: HY-173083CAS No.: 1103840-28-3MDA7 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.
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MN-25
0 ImagesCat. No.: HY-124954CAS No.: 501926-82-5MN-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].
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TRPM8 antagonist 4 prodrug
0 ImagesCat. No.: HY-174846TRPM8 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.
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L-759656
0 ImagesCat. No.: HY-110041CAS No.: 174627-56-6L-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.
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VU6077967
0 ImagesCat. No.: HY-181636VU6077967 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.
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CB1/2 receptor-1
0 ImagesCat. No.: HY-164817CAS No.: 1260669-31-5CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.
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CB2R probe 1
0 ImagesCat. No.: HY-147532CAS No.: 2634714-79-5CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells.
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(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide
0 ImagesCat. No.: HY-115428CAS No.: 220556-74-1(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 Kis of both 21 μM.
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Dodec-2E-ene-8,10-diynoic acid isobutylamide
0 ImagesCat. No.: HY-N19807CAS No.: 120727-29-9Dodec-2E-ene-8,10-diynoic acid isobutylamide is an alkamide found in Echinacea angustifolia that binds to CB1 (rat Ki = 61.1 μM) and CB2 (mouse Ki = 47.2 μM) cannabinoid receptors. Dodec-2E-ene-8,10-diynoic acid isobutylamide can be used in research on inflammatory diseases.
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CB2 receptor agonist 6
0 ImagesCat. No.: HY-163394CB2 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.
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CB2R/FAAH modulator-2
0 ImagesCat. No.: HY-152253CAS No.: 2876918-68-0CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki 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.
