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Cat. No. Product Name CAS No. Information
PC-60146

APD-371

1268881-20-4

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.

Pain

Phase 2 Clinical

PC-60086

AM-6538

1245626-00-9

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

PC-35625

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.
PC-35592

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.
PC-35536

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.
PC-35488

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.
PC-35485

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.

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