VCE-004.3

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.

References 1. Del Rio C, et al. Br J Pharmacol. 2018 Jul 22. doi: 10.1111/bph.14450. View Related Products by Target Cannabinoid Receptor