Catalog No.
Product Name
Application
Product Information
Citations
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PDK Inhibitor, CB1/CB2 Agonist
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor, demonstrating an IC50 value of 9.5 μM. It effectively lowers blood glucose levels in diabetic mouse models. Additionally, Leelamine acts as a weak agonist of cannabinoid receptors CB1 and CB2. Its biological activity includes a reduction in mitotic activity and prostate-specific antigen expression, as well as the induction of apoptosis in cancer cells, making it a valuable tool for cancer research and metabolic studies. -
CB2 Receptor Agonist
Tetrahydromagnolol, a potent and selective agonist of the cannabinoid CB2 receptor, exhibits an EC50 value of 170 nM. It has a binding affinity (Ki) for the CB2 receptor of 416 nM, which is significantly higher compared to the CB1 receptor. This compound demonstrates notable biological activities, including antifungal, anti-inflammatory, and analgesic effects, making it valuable for research in pain management and inflammatory disorders. Additionally, its role as a GPR55 antagonist further enhances its potential utility in cannabinoid-related studies. -
Cannabinoid Receptor Inhibitor
2-Linoleoyl glycerol is a monoacylglycerol that serves as an antagonist and partial agonist at the cannabinoid receptor type 1 (CB1). It effectively modulates the activity of cannabinoids such as anandamide (AEA) and 2-arachidonoylglycerol (2-AG) by attenuating their effects without enhancing them. This compound has significant implications in cannabinoid research, particularly in studies focused on the endocannabinoid system and potential therapeutic targets for various conditions. Additionally, its potency can be influenced by the inhibition of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). -
CB1 Agonist
CB1 agonist 1 is a potent agonist of the cannabinoid receptor type 1 (CB1). With a pIC50 value of 5.7, it exhibits significant binding affinity to the CB1 receptor. This compound is primarily utilized in research focusing on brain disorders, aiding in the exploration of cannabinoid signaling and its implications in neurological conditions. -
GPR18 Agonist
PSB-KK1445 is a potent and selective GPR18 agonist, exhibiting EC50 values of 45.4 nM for human GPR18 and 124 nM for mouse GPR18. It demonstrates over 200-fold selectivity against both cannabinoid receptor subtypes, GPR55, and GPR183. This compound is valuable for research applications exploring the physiological roles of GPR18 in various biological processes and potential therapeutic uses related to the endocannabinoid system. -
Cannabinoid Receptor Antagonist
O1918 is a selective antagonist of the cannabinoid receptor GPR18. It effectively inhibits GPR18 signaling, making it a valuable tool for studying the role of this receptor in various physiological processes. O1918 is primarily used in research focusing on cannabinoid modulation and its effects on the endocannabinoid system. -
CB1 Antagonist
AM281 is a selective antagonist of the cannabinoid receptor type 1 (CB1) with an IC50 value of 9.91 nM. This compound exhibits significant potency in inhibiting the CB1 receptor, while demonstrating a much lower affinity for the CB2 receptor with an IC50 of 13,000 nM. AM281 is primarily utilized in research applications related to endocannabinoid signaling, neurobiology, and the potential modulation of disorders involving CB1 receptor activity. -
CB1 Receptor Antagonist
AM6545 is a highly selective CB1 receptor antagonist that functions peripherally without crossing the blood-brain barrier (Ki=1.7 nM). By competitively inhibiting the CB1 receptors, AM6545 disrupts endocannabinoid signaling, thereby mitigating appetite stimulation and inflammatory responses without altering cAMP levels. This compound has been shown to significantly decrease food intake and body weight in murine models while improving metabolic syndrome-related renal impairment, including proteinuria, fibrosis, and insulin resistance. AM6545 is instrumental in research focused on obesity and its associated complications. -
CB1/2 Agonist
CB1/2 Agonist 3 is a potent non-selective cannabinoid receptor agonist targeting both CB1 and CB2 receptors. With Ki values of 5.9 nM for hCB1 and 3.5 nM for hCB2, this compound exhibits significant binding affinity. It is instrumental in studying cannabinoid signaling pathways and their implications in various biological processes and therapeutic areas. -
VR1/CB1 Ligand
Arvanil is a selective ligand for the vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1). It exhibits potent neuroprotective properties and has been shown to inhibit spasticity. This compound is of interest in research applications focused on pain management, neuroprotection, and the modulation of endocannabinoid signaling pathways. -
CB1 Receptors Agonist
Arachidonylcyclopropylamide (ACPA) is a highly selective agonist of the CB1 receptors. It effectively inhibits forskolin-stimulated cAMP production in Chinese hamster ovary (CHO) cells expressing human cannabinoid CB1 receptors, exhibiting an IC50 of 2 nM. ACPA is widely utilized in research to investigate the role of endocannabinoids in physiological processes and the therapeutic potential of cannabinoid modulation. -
Stable Isotope
2-Arachidonoylglycerol-d8 is a deuterated analog of 2-Arachidonoylglycerol, a natural endocannabinoid that acts as a ligand for cannabinoid receptors in the central nervous system. This stable isotope is utilized in biochemical and pharmacological research to study cannabinoid signaling and interactions. Its application includes mass spectrometry-based analysis, enabling precise quantification of endocannabinoid levels in biological samples for further investigation of their physiological roles. -
CB1/2 agonist
CB1/2 Agonist 1 is a selective cannabinoid receptor agonist, targeting both CB1 and CB2 receptors with EC50 values of 56.15 nM and 11.63 nM, respectively. This compound effectively reduces glutamate release and LPS-induced microglial cell activation, demonstrating significant anti-inflammatory and antinociceptive properties. Due to its unique pharmacological profile, CB1/2 Agonist 1 has potential applications in research related to multiple sclerosis and other neuroinflammatory conditions. -
Cannabinoid Antagonist
AM-6538 is a high-affinity, pseudo-irreversible cannabinoid (CB) antagonist that serves as a valuable tool for research on cannabinoid receptor modulation. As a structural analog of rimonabant, it effectively evaluates the efficacy of both full and partial agonists at cannabinoid receptors. Additionally, AM-6538's unique alkyne group allows it to function as a click chemistry reagent, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This makes it suitable for applications that require temporary modulation of cannabinoid receptor availability. -
CB1 Agonist
(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays. -
CB2Rs Positive Allosteric Modulator
CB2R PAM is a positive allosteric modulator of cannabinoid type-2 receptors (CB2Rs) with oral bioavailability. This compound exhibits significant antinociceptive activity, demonstrated in vivo in mouse models of neuropathic pain. CB2R PAM offers valuable insights for research applications related to pain management and cannabinoid pharmacology. -
CB2 Receptor Agonist
GW 833972A is a selective agonist of the CB2 receptor, exhibiting a pEC50 value of 7.3 for human CB2. With approximately 1000-fold higher selectivity for the CB2 receptor over CB1, GW 833972A effectively inhibits induced neuronal depolarization and alleviates cough reflex in guinea pig models. This compound is valuable for research into chronic cough mechanisms and potential therapeutic interventions. -
CB1 Receptor Antagonist
CB1 antagonist 4 is a selective inverse agonist for the cannabinoid receptor 1 (CB1), demonstrating an IC50 of 8.5 nM in human CB1 assays. This compound exhibits a notable selectivity for CB1 over CB2 receptors, with an IC50 of 604.9 nM. CB1 antagonist 4 effectively inhibits GTP binding in CB1-overexpressing cell membranes, with an EC50 of 18.5 nM, making it a valuable tool for studying CB1 receptor biology and signaling pathways. -
CB1 Antagonist
Ibipinabant is a potent and selective antagonist of the cannabinoid CB1 receptor, exhibiting a Ki value of 7.8 nM. This compound demonstrates over 1000-fold selectivity for CB1 compared to CB2, with a Ki of 7943 nM. Ibipinabant is primarily utilized in research related to obesity and diabetes, facilitating studies on the modulation of appetite and metabolic regulation. -
CB1/CB2 Receptor Agonist
Eicosapentaenoyl ethanolamide is a cannabinoid receptor agonist targeting the CB1 and CB2 receptors. This omega-3 fatty acid, classified as a N-acylethanolamine, serves as a crucial metabolic signal. Research demonstrates that eicosapentaenoyl ethanolamide inhibits lifespan extension induced by dietary restriction in wild-type organisms and additionally suppresses lifespan extension in TOR pathway mutants. Its applications include studies in metabolism, aging, and cannabinoid receptor signaling. -
Cannabinoid Receptor Agonist
Dihomo-γ-Linolenoyl Ethanolamide is a potent cannabinoid receptor agonist, selectively targeting human recombinant CB1 and CB2 receptors with inhibition constants (Kis) of 857 nM and 598 nM, respectively. This endocannabinoid plays a crucial role in modulating various physiological processes, making it relevant for studies in pain management, inflammation, and neuroprotection. Its unique mechanism of action positions it as a valuable tool for cannabinoid research and therapeutic exploration. -
CB1 Antagonist
Drinabant is a potent antagonist of the CB1 receptor, specifically designed for oral activity. It effectively inhibits agonist-stimulated calcium signaling, demonstrating IC50 values of 25 nM for human CB1 receptors and 10 nM for rat CB1 receptors, while showing no efficacy against human CB2 receptors. This compound is valuable for research applications involving the endocannabinoid system and its role in various physiological processes. -
CB2 Agonist
SCH 336 is a potent and selective inverse agonist of the CB2 receptor. It has been shown to inhibit the migration of BaF3 cells expressing CB2, as well as significantly reduce leukocyte migration in vivo. Additionally, SCH 336 effectively blocks ovalbumin-induced eosinophilia in mouse models, making it a valuable tool for research into inflammation and immune response modulation. -
CB1 Agonist
CB1 inverse agonist 2 is a potent orally active inverse agonist targeting the Cannabinoid Receptor CB1. This compound effectively inhibits CP55940-induced hypothermia and anorexia in mouse models, making it a valuable tool for studying cannabinoid receptor-mediated pathways. Its ability to modulate CB1 receptor activity positions it as a significant reagent for research in neuropharmacology and metabolic disorders. -
CB1 Agonist
2-Palmitoylglycerol is a cannabinoid receptor CB1 agonist that shows modest binding affinity. This compound is closely related to 2-arachidonoylglycerol and may also act as an endogenous ligand for the GPR119 receptor. Its research applications include studying cannabinoid signaling pathways and exploring potential therapeutic implications in neurobiology and metabolic disorders. -
CB1/CB2 Receptor Agonist
AZD1940 is a high-affinity agonist for the cannabinoid receptors CB1 and CB2, exhibiting pKi values of 7.93 and 9.06, respectively. This compound demonstrates significant analgesic activity, making it a valuable tool for studying pain pathways and cannabinoid signaling. Its oral bioactivity encourages research applications in neuropharmacology and potential therapeutic development for pain management. -
Cannabinoid Receptor Agonist
VSN-16 is a potent cannabinoid receptor agonist that exhibits vasodilatory activity. This compound is valuable for investigating the role of cannabinoid signaling in various physiological processes and has potential applications in the study of multiple sclerosis and related neuroinflammatory conditions. Its ability to modulate vascular responses makes it a useful tool for researchers examining therapeutic strategies in this area. -
CB1 Receptor Antagonist
Zevaquenabant ((S)-MRI-1867) is a peripherally restricted antagonist of the cannabinoid CB1 receptor and inducible nitric oxide synthase (iNOS). This compound has demonstrated potential in ameliorating obesity-induced chronic kidney disease (CKD), making it useful for research applications focused on metabolic disorders and renal pathologies. Its oral bioavailability enhances its utility in preclinical studies aimed at evaluating therapeutic strategies for obesity-related complications. -
Cannabinoid Receptor Antagonist
Hemopressin (human, mouse) is a nonapeptide that functions as an inverse agonist of the CB1 cannabinoid receptors. Originally derived from the α1-chain of hemoglobin and isolated from rat brain homogenates, Hemopressin is orally active and exhibits selective antagonistic properties. This compound demonstrates significant antinociceptive effects in models of inflammatory pain, making it a valuable tool for research into pain mechanisms and cannabinoid receptor biology. -
CB1 PAM
ZCZ011 is a potent positive allosteric modulator of the cannabinoid 1 (CB1) receptor. It enhances the binding of CP55,940 to CB1 receptors and stimulates anandamide (AEA)-mediated GTPγS binding in mouse brain membranes. ZCZ011 also promotes β-arrestin recruitment and ERK phosphorylation in human CB1 cells, making it a valuable tool for investigating mechanisms associated with neuropathic and inflammatory pain. -
CB2 Receptor Agonist
CB2 receptor agonist 2 is a highly potent and selective agonist for the cannabinoid type 2 (CB2) receptor, exhibiting a binding affinity with a Ki value of 8.5 nM. This compound serves as a valuable tool for investigating the role of CB2 in various biological processes such as inflammation and neuroprotection. Its specificity for the CB2 receptor makes it suitable for research applications focused on cannabinoid signaling pathways and potential therapeutic interventions. -
Cannabinoid Receptor Antagonist
CB1-IN-1 is a selective cannabinoid receptor type 1 (CB1R) antagonist, demonstrating a potent inhibition with a Ki value of 0. Its peripherally restricted mechanism of action makes it particularly valuable for studies investigating the physiological roles of CB1R in peripheral tissues. CB1-IN-1 is applicable in research focused on metabolic disorders, pain management, and neuroprotection, facilitating the exploration of therapeutic interventions targeting the endocannabinoid system. -
CB2 Agonist
Vicasinabin (RG7774) is an orally active, selective full agonist of the cannabinoid receptor type 2 (CB2R), exhibiting EC50 values of 2.81 nM for human CB2R and 2.60 nM for mouse CB2R. By selectively activating CB2R, Vicasinabin effectively inhibits inflammatory responses, reduces leukocyte adhesion, and decreases vascular permeability. This compound is valuable for research focused on conditions such as diabetic retinopathy, uveitis, and laser-induced choroidal neovascularization. -
Cannabinoid Receptor Antagonist
Hemopressin (rat) is a nonapeptide derived from the α1-chain of hemoglobin, known for its role as a selective inverse agonist of the CB1 cannabinoid receptors. This compound demonstrates antinociceptive effects in various inflammatory pain models, making it a valuable tool for research on pain mechanisms and cannabinoid signaling. Its oral bioactivity enhances its utility in in vivo studies within the field of cannabinoid pharmacology. -
Cannabinoid Receptor Modulator
JTE-907 is a highly selective cannabinoid receptor modulator that acts as an inverse agonist at the CB2 receptor. This compound demonstrates notable anti-inflammatory activity in vivo, making it valuable for research in inflammation-related pathways. Its unique mechanism positions JTE-907 as a useful tool for elucidating the role of CB2 receptors in various biological processes and for exploring potential therapeutic applications in inflammatory diseases. -
CB1 Receptor Antagonist
URB447 is a peripherally restricted antagonist of the CB1 receptor, exhibiting an IC50 of 313 nM for rat CB1 and 41 nM for human CB2 receptors. This compound effectively reduces food intake and body weight gain in murine models by circumventing the central nervous system, thereby not interfering with central CB1-mediated responses. URB447 serves as a valuable tool for obesity research, providing insights into the peripheral modulation of cannabinoid signaling. -
CB1 Ligand
CB-25 is a partial agonist of the CB1 cannabinoid receptor. It has been shown to enhance Forskolin-induced cAMP formation specifically in cancer cells, while not affecting hCB1-CHO cells. This compound serves as a valuable tool for investigating the role of cannabinoid signaling pathways in cancer biology and related research applications. -
CB1R Allosteric Modulator
CB1R Allosteric Modulator 5 is a selective allosteric modulator targeting the Cannabinoid receptor type 1 (CB1R) with a pIC50 of 6.89. This compound effectively reduces cocaine-seeking behavior associated with cue-induced reinstatement and mitigates cocaine-induced behavioral sensitization, while leaving locomotor activity unaffected. It is suitable for research applications concerning addiction, neuropharmacology, and the modulation of cannabinoid signaling pathways. -
Cannabinoids Precursor
(1H-Indol-3-yl)(2,2,3,3-tetramethylcyclopropyl)methanone serves as a key precursor in the synthesis of synthetic cannabinoids. This compound is integral for the development of potent cannabinoid receptor modulators, facilitating research into cannabinoid pathways and their physiological effects. It is valuable for studies focused on cannabinoid-related pharmacology and drug development. -
CB2R Antagonist
PGN36 is a selective antagonist of the cannabinoid CB2 receptor (CB2R), with a Ki of 0.09 µM for CB2R and >40 µM for CB1R. This compound effectively inhibits the upregulation of collagen type I gene expression induced by promoters of bone metabolism. Notably, PGN36 is capable of crossing the blood-brain barrier, making it a valuable tool for studying frontotemporal dementia (FTD) and other neurological conditions. -
Stable Isotope
Linoleoyl ethanolamide-d4 is a deuterated analog of Linoleoyl ethanolamide, targeting cannabinoid receptors type-1 (CB1) and type-2 (CB2). This compound exhibits weak binding affinity, with inhibition constants (Kis) of 10 μM and 25 μM for CB1 and CB2, respectively. It is utilized in biochemical research to investigate cannabinoid receptor dynamics and efficacy in functional assays. Additionally, Linoleoyl ethanolamide-d4 serves as a useful tool in studies exploring fatty acid ethanolamides and their biological effects. -
CB2 receptor Agonist
A-836339 is a selective agonist of the CB2 receptor, demonstrating Ki values of 0.4 nM and 0.8 nM for human and rat CB2 receptors, respectively. It exhibits significant analgesic, anti-inflammatory, gastric protective, and antioxidant activities. Activation of CB2 receptors in the dorsal root ganglia and spinal cord mediates its antinociceptive properties. Additionally, A-836339 reduces pro-inflammatory cytokines like TNF-α and IL-1β while enhancing the activity of antioxidant enzymes such as catalase and superoxide dismutase. This compound is valuable for research into inflammatory pain, neuropathic pain, gastric ulcers, and cerebral ischemia. -
CB1 Inhibitor
ANEB-001 is an orally active inhibitor of the cannabinoid receptor type 1 (CB1). This compound is primarily utilized in research focused on acute cannabinoid intoxication, providing insights into the physiological effects and potential therapeutic approaches related to CB1 modulation. Its selective inhibition of CB1 makes it a valuable tool for studies investigating cannabinoid-related pathways and their implications in various biological contexts. -
CB2 Receptor Agonist
LEI-101 is a selective, orally bioavailable agonist of the cannabinoid CB2 receptor, exhibiting a pEC50 of 8 for human CB2. With a pKi of less than 4 for hERG, it demonstrates minimal off-target activity. This compound is approximately 100-fold more potent in binding to CB2 receptors compared to CB1 receptors, making it a valuable tool for research in pain modulation, inflammation, and neuroprotection studies. -
CB2 Selective Agonist
CB65 is a selective agonist for the CB2 receptor, demonstrating potent activity with a Ki value of 3.3 nM. Its affinity for the CB1 receptor is significantly lower, with a Ki value exceeding 1000 nM. This compound is primarily utilized in research focused on cannabinoid receptor signaling pathways and has potential applications in studying inflammation and pain modulation. -
Endocannabinoid Analog
Docosahexaenoyl glycerol is an analog of the endocannabinoid system that primarily targets cannabinoid receptors. This compound enhances glucose uptake and demonstrates anti-inflammatory properties, making it a valuable tool for research in metabolic and inflammatory disorders. Its utility extends to studies exploring the interplay between endocannabinoids and energy metabolism, providing insights into potential therapeutic applications. -
GPR55 Antagonist
PSB-SB-487 is a potent antagonist of GPR55, exhibiting an IC50 value of 0.113 µM, and acts as an agonist for the CB2 receptor with a Ki value of 0.292 µM. This compound is valuable for investigating various biological processes and disease states, including diabetes, Parkinson’s disease, neuropathic pain, and cancer. Its dual activity makes it a significant tool for understanding the role of cannabinoid receptors in disease mechanisms and potential therapeutic interventions. -
CB2 Receptor Agonists
CB2 receptor agonist 10 specifically targets the cannabinoid receptor type 2 (CB2) with a Ki of 3.7 nM for human CB2 and a Ki of 110 nM for human CB1. It exhibits a potent EC50 of 0.52 nM for hCB2, indicating its high efficacy in activating this receptor. This compound is primarily utilized in research applications focused on cannabinoid signaling pathways, inflammation, and neuroprotection. -
CB2 Agonist
GP1a is a potent agonist of the cannabinoid receptor 2 (CB2), demonstrating significant anti-inflammatory properties. This compound is effective in promoting skin wound healing by inhibiting inflammation and fibrogenesis, while facilitating the process of re-epithelialization. GP1a is valuable for research applications related to tissue repair and inflammation regulation. -
CB1 antagonist
MJ15 is a potent and selective antagonist of the cannabinoid receptor type 1 (CB1), with a Ki of 27.2 pM and an IC50 of 118.9 pM specifically for rat CB1 receptors. This compound has demonstrated significant biological activity in models of obesity and hyperlipidemia, effectively inhibiting food intake and preventing increases in body weight in diet-induced obese rats and mice. MJ15 is valuable for research applications focused on metabolic disorders and the endocannabinoid system.
