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You are here:Home-Inhibitors & Agonists-GPCR-Cannabinoid Receptor

Request The Product List ofCannabinoid Receptor Cannabinoid Receptor

Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Cat. No. Product Name CAS No. Information
GY03989

Iodopravadoline

164178-33-0

A potent and selective inverse agonist for the cannabinoid receptor CB2 with Ki of 32.1 nM, 165-fold selectivity over CB1; inhibits forskolin-stimulated cyclic AMP production in CB1-transfected cells (22.6% at 1 uM and 45.9% at 10 uM).

GY06945

AM-6538

1245626-00-9

AM-6538 (AM6538) is a potent, selective cannabinoid receptor CB1 antagonist with Ki of 5.1 nM.

GY06923

XL-001

1426153-46-9

XL-001 (XL001) is a novel specific CB2 inverse agonist with Ki of 0.5 nM; inhibits in a dose-dependent fashion the fibrogenic response induced by CB2 overexpression, CB2 agonist or transforming growth factor-β1, ameliorates kidney injury, fibrosis and inflammation in both the obstruction and ischemia/reperfusion models.

GY06879

VCE-004.3

1818428-14-6

VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61); binds to an alternative site at the PPARγ ligand-binding pocket (LBP); VCE-004.3 inhibits collagen gene transcription and synthesis and prevents TGFβ-induced fibroblast migration and differentiation to myofibroblasts; VCE-004.3 prevents skin fibrosis, myofibroblast differentiation and ERK1/2 phosphorylation in bleomycin-induced skin fibrosis; reduces mast cell degranulation, macrophage activation, T lymphocytes infiltration, and the expression of inflammatory and profibrotic factors.

GY06854

GAT-100

1663564-42-8

GAT-100 (GAT100) is a potent, selective CB1R negative allosteric modulator (NAM) with cAMP EC50 and β-arr EC50 of 174 nM and 2.1 nM, does not exhibit inverse agonism; GAT-100 is a covalent probe for mapping structure-function correlates characteristic of the druggable CB1R allosteric space.

GY06851

GAT-211

102704-40-5

GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM; engages CB1R allosteric site(s), enhances the binding of the orthosteric full agonist [3H]CP55,490, and reduces the binding of the orthosteric antagonist/inverse agonist [3H]SR141716A; displayed both PAM and agonist activity in HEK293A and Neuro2a cells expressing human recombinant CB1R (hCB1R) and in mouse-brain membranes rich in native CB1R.

GY06722

AM9405

AM9405 (AM-9405, GAT-379) is novel potent, peripherally active cannabinoid type 1 (CB1) and 5-HT3 receptor agonist, inhibits the EFS-induced twitch contraction of the ileum and the colon with IC50 of 0.076 and 45.71 nM, respectively; significantly slows mouse intestinal motility in physiological conditions, reverses hypermotility and reduced pain in mouse models mimicking symptoms of functional GI disorders, such as stress-induced diarrhea and writhing test.

GY04077

CP-945598

686347-12-6

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.

GY04041

CP945598

686344-29-6

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.

GY03233

Bay 59-3074

406205-74-1

Bay 59-3074 is a potent, selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 48.3, and 45.5 nM for human CB1 and human CB2 receptors, respectively; displays antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic; orally acitve.

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