Tapinarof CAS# 79338-84-4 苯烯莫德

Benvitimod (also known as tapinarof, GSK2894512, or WBI-1001) is a naturally derived small-molecule aryl hydrocarbon receptor (AhR) agonist that has shown potent anti-inflammatory and antioxidant effects in preclinical studies. In vitro, benvitimod activated AhR signaling in keratinocytes and dendritic cells with an EC₅₀ in the low nanomolar range (~10–30 nM), inducing expression of downstream targets such as CYP1A1 and Nrf2-dependent antioxidant genes while suppressing proinflammatory cytokines including IL-17A, IL-22, and TNF-α. In murine models of psoriasis-like dermatitis induced by imiquimod, topical benvitimod significantly reduced erythema, scaling, and epidermal hyperplasia, with over 80% reduction in IL-17A mRNA and normalization of epidermal thickness to near-baseline levels after 7 days of treatment. Similarly, in atopic dermatitis models, benvitimod attenuated Th2 cytokine (IL-4, IL-13) expression and reduced inflammatory cell infiltration by 60–70% compared with vehicle.