887375-26-0

887375-26-0 structure

Name: Mapracorat
Chemical Name: (2R)-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-[[(2-methylquinolin-5-yl)amino]methyl]pentan-2-ol
CAS Number: 887375-26-0
Molecular Formula: C₂₅H₂₆F₄N₂O₂
Molecular Weight: 462.48000
Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
Create Date: 2018-06-21 17:31:00
Modify Date: 2024-01-02 10:29:58
Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.

Name	(2R)-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-[[(2-methylquinolin-5-yl)amino]methyl]pentan-2-ol
Synonyms	Mapracorat UNII-145V79YBVP

Description	Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor Research Areas >> Endocrinology
In Vitro	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%) and triamcinolone acetonide (0.015%) led to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas. However, once daily topical administration of triamcinolone acetonide significantly reduced skin fold thickness from day 8 to 14, whereas no such reduction was observed for mapracorat.
References	[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. [2]. Baiula M, et al. Mapracorat, a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis.Inflamm Allergy Drug Targets. 2014; 13(5):289-98.