Mapracorat

Modify Date: 2025-08-29 11:16:11

Use of Mapracorat

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
Synonym	More Synonyms

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.

Molecular Formula	C₂₅H₂₆F₄N₂O₂
Molecular Weight	462.48000
Exact Mass	462.19300
PSA	54.38000
LogP	5.76340
InChIKey	VJGFOYBQOIPQFY-XMMPIXPASA-N
SMILES	Cc1ccc2c(NCC(O)(CC(C)(C)c3cc(F)cc4c3OCC4)C(F)(F)F)cccc2n1
Storage condition	2-8℃

Mapracorat

UNII-145V79YBVP

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Price: ￥7150/10 mM * 1 mL in DMSO

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