Catalog No.
Product Name
Application
Product Information
Citations
- Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.
- Marie-Eve Di Raddo, .et al. , Curr Res Neurobiol, 2023, Sep 4:5:100107 PMID: 38020805
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CB1 receptor inverse agonist
Rimonabant hydrochloride is a CB1 receptor inverse agonist. -
CB1 receptor inverse agonist
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro. -
CB receptor agonist
WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.- Vida mirzaie, .et al. , Research Square, 2024, October
- Greish K, .et al. , J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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CB2 receptor agonist
Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials. -
CB1/CB2 receptor agonist
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . -
CB1 antagonist
CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM. -
CB1 agonist
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. -
CB-1 receptor antagonist
(±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM. -
CB1 antagonist/inverse agonist
Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1. -
CB1 receptor inverse agonist
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist. -
immune modulator
Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55). -
GPR18 Agonist
N-Arachidonylglycine (NA-Gly) selectively acts as an agonist for the GPR18 receptor, exhibiting an EC50 value of 44.5 nM. Unlike its structural analog anandamide, NA-Gly does not engage with CB1 or CB2 receptors. This compound also demonstrates inhibitory activity on GLYT2 with an IC50 of 5.1 μM. Additionally, N-Arachidonylglycine has been shown to effectively promote the migration of endometrial cells, making it a valuable tool for research in cellular migration and cannabinoid receptor activity. -
Anticancer Agent
Auriculasin is an anticancer agent that primarily targets VEGFR2, PI3K/AKT/mTOR, and MAPK signaling pathways. It effectively inhibits cell proliferation, induces apoptosis, and suppresses angiogenesis, while also promoting mitochondrial oxidative stress and ferroptosis. Additionally, Auriculasin demonstrates activity at the cannabinoid receptor CB1 with an IC50 of 8.92 μM. This compound is valuable for cancer research, particularly in studying prostate cancer, non-small cell lung cancer, and the development of anti-angiogenic therapies. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
CB2 Agonists
MN-25 is an orally active indolpyridone that functions as a selective CB2 agonist, exhibiting a Ki of 245 nM for CB1 and a potent 11 nM for CB2. This compound demonstrates significant anti-inflammatory properties by inhibiting TNF-R release in human peripheral blood mononuclear cells in vitro, with an IC50 of 33 μM. In vivo studies have shown that MN-25 is effective in reducing acute inflammation in a mouse model at oral doses up to 50 mg/kg, making it a valuable reagent for exploring cannabinoid receptor biology and therapeutic applications in inflammation. -
CB2 Agonist
GW405833 hydrochloride is a selective agonist of the cannabinoid receptor 2 (CB2) with potent activity, characterized by EC50 and Ki values of 0.65 nM and 3.92 nM, respectively. In addition to its action as a CB2 agonist, GW405833 also acts as a non-competitive antagonist at the CB1 receptor, influencing analgesic pathways. This compound has been shown to significantly inhibit cAMP production stimulated by Forskolin and to down-regulate HIF-1α, which contributes to its potential role in alleviating acute liver failure. GW405833 hydrochloride is valuable for research related to pain management and metabolic disorders. -
CB2 Agonist
GW-405833 is a selective agonist of the cannabinoid receptor 2 (CB2), with an EC50 value of 0.65 nM. It exhibits a strong affinity for CB2, while displaying significantly lower activity at CB1, with EC50 and Ki values of 16.1 μM and 4772 nM, respectively. In addition to its agonistic effects at CB2, GW-405833 acts as a non-competitive antagonist at CB1, mediating analgesic and anti-inflammatory effects. Furthermore, it inhibits forskolin-stimulated cAMP production and down-regulates HIF-1α, potentially alleviating acute liver failure through modulation of glycolysis. This compound is useful for research in pain management, inflammation, and liver pathology. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. -
Cannabinoid Receptor Inhibitor
Yangonin is a selective cannabinoid receptor inhibitor that demonstrates affinity for the human recombinant CB1 receptor, with an IC50 value of 1.79 μM and a Ki of 0.72 μM. This compound is of significant interest for research applications aimed at understanding cannabinoid signaling and its implications in various physiological processes. Its modulation of CB1 receptor activity may provide insights into therapeutic strategies targeting cannabinoid-related pathways. -
CB1 Antagonist
LY320135 is a potent and selective antagonist of the cannabinoid receptor type 1 (CB1) with a Ki of 141 nM. It also exhibits binding affinity for 5-HT2 and muscarinic receptors, with Kis of 6.4 μM and 2.1 μM, respectively. This compound demonstrates neuroprotective effects and is useful in studies related to neurodegeneration and cannabinoid signaling pathways. -
Endocannabinoid
Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies. -
CB2R Agonist
CB2R agonist 4 is a selective agonist for the cannabinoid receptor 2 (CB2R), exhibiting an EC50 value of 6.9 μM. This compound can induce cellular apoptosis, promote reactive oxygen species (ROS) production, and contribute to protein misfolding. Due to its cytotoxic effects observed in various tumor cell lines, CB2R agonist 4 is a valuable tool for cancer research applications. -
Stable Isotope
Yangonin-d3 is a deuterium-labeled derivative of Yangonin, acting as a stable isotope. This compound demonstrates binding affinity for the human recombinant cannabinoid CB1 receptor, with an IC50 of 1.79 μM and a Ki of 0.72 μM. Yangonin-d3 is valuable for research applications in cannabinoid receptor studies, enabling the exploration of receptor mechanisms and the development of cannabinoid-based therapeutics. -
CB1 Antagonist/PPARα Agonist
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. This compound demonstrates notable activity in inhibiting alcohol intake with an EC50 value of 0.2 mg/kg. Additionally, OLHHA effectively reduces hepatic lipid accumulation and circulating triglyceride levels, exhibiting anti-steatotic properties. Its mechanism and effects make it a valuable tool for research into non-alcoholic fatty liver disease (NAFLD). -
CB1 Receptor Inhibitor
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a selective inhibitor of the cannabinoid CB1 receptor. This neurosteroid, a key precursor in steroid hormone synthesis, can mitigate the effects of tetrahydrocannabinol (THC) by blocking its action at CB1 receptors. Additionally, Pregnenolone monosulfate sodium serves as a TRPM3 channel activator and has been shown to weakly activate TRPM1 channels. Its unique properties make it a valuable tool for investigating cannabinoid signaling and neuroprotective strategies against cannabis-related effects. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a selective inhibitor of the cannabinoid CB1 receptor. By inhibiting the effects of tetrahydrocannabinol (THC) mediated through the CB1 receptors, it offers potential neuroprotective properties against cannabis intoxication. Additionally, Pregnenolone monosulfate serves as a TRPM3 channel activator and exhibits weak activation of TRPM1 channels, making it valuable for research in neuropharmacology and cannabinoid signaling pathways. -
Stable Isotope
Rimonabant-d10 is a deuterium-labeled analog of Rimonabant, a highly potent and selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound not only exhibits strong brain penetration but also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant-d10 serves as a valuable tool for studying cannabinoid receptor signaling and the role of CB1 in various biological processes, as well as for applications in mycobacterial research.
