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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
34 Results for "
human CB1
" in MedChemExpress (MCE) Product Catalog:
Products (34)
34 Results for "human CB1" in MCE Product Catalog:
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Otenabant 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.
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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.
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Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) .
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other families Other Phenylpropanoids Phenylpropanoids Plants Disease Research Fields Inflammation/Immunology
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1 Cited Publications
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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 .
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CB1 antagonist 4 (compound 8) is a selective cannabinoid receptor 1 (CB1) inverse agonist with an IC50 of 8.5 nM for human CB1. CB1 antagonist 4 shows selective for CB1 over CB2 receptors (IC50 of 604.9 nM). CB1 antagonist 4 inhibits GTP binding to CB1-overexpressing cell membranes with an EC50 of 18.5 nM .
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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 .
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JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis .
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2-Linoleoyl glycerol (2-Monolinolein) is a partial CB1 receptor agonist with a pEC50 of 4.781. 2-Linoleoyl glycerol activates the hCB1 receptor. 2-Linoleoyl glycerol does not induce an increase in intracellular free Ca 2+. 2-Linoleoyl glycerol can be used in the research of neurological disorders .
Cat. No.: HY-177425
CAS No.: 152674-95-8
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AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 Ki of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity .
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O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels .
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URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity .
Cat. No.: HY-159161
CAS No.: 2237222-16-9
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PSB-CB-27 is a potent and selective GPR18 inhibitor with an IC50 of 0.65 μM. PSB-CB-27 shows selectivity over Human GPR55, Human CB1 receptor, and Human CB2 receptor. PSB-CB-27 leads to a complete blockade of Δ9-Tetrahydrocannabinol (THC)-induced GPR18 activation. PSB-CB-27 can be used for inflammatory diseases and cancer immunotherapy research .
Cat. No.: HY-112828
CAS No.: 1800327-36-9
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LEI105 is a highly selective and reversible diacylglycerol lipase (DAGL) inhibitor that exhibits significant inhibitory activity against human DAGLα and DAGLβ (e.g., the pIC50 value against human DAGLα is 8.5, and the IC50 against human DAGLβ is 32 nM). LEI105 effectively reduces intracellular 2-arachidonoylglycerol levels and inhibits CB1 receptor-mediated short-term synaptic plasticity. LEI105 can be used to investigate the on-demand biosynthesis of 2-AG in retrograde signaling .
Cat. No.: HY-10871A
CAS No.: 686347-12-6
Synonyms: CP 945598 Hydrochloride
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Otenabant Hydrochloride 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.
Cat. No.: HY-152581
Purity: 98.08%
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CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines .
Cat. No.: HY-152576
CAS No.: 1817633-49-0
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CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
Cat. No.: HY-172568
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(±)5(6)-EET Ethanolamide is a metabolite of Anandamide (HY-10863) generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
