(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
(S)-Mapracorat concentration dependently inhibited TNFα secretion from activated canine PBMC with IC50 value of approximately 0.2 nM.
Intradermal injection of compound 48/80 (50 μg in 50 μL saline) resulted in a clear wheal and flare reaction over the 60 min observation period. Topical pre-treatment with (S)-Mapracorat (0.1%) leads to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas.
[1]. BÄumer W , et al. The selective glucocorticoid receptor agonist mapracorat displays a favourable safety-efficacy ratio for the topical treatment of inflammatory skin diseases in dogs. Vet Dermatol. 2017 Feb; 28(1):46-e11.