| Bioactivity | Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist. | ||||||||||||
| Invitro | Mapracorat concentration dependently inhibited TNFα secretion from activated canine PBMC with IC50 value of approximately 0.2 nM. | ||||||||||||
| In Vivo | 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 mapracorat (0.1%) leads to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas. | ||||||||||||
| Name | Mapracorat | ||||||||||||
| CAS | 887375-26-0 | ||||||||||||
| Formula | C25H26F4N2O2 | ||||||||||||
| Molar Mass | 462.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |