Mapracorat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mapracorat (ZK 245186) 是一种有效的、选择性的非类固醇糖皮质激素受体 (GR) 激动剂，结合 Ki 为 1.9 nM。

Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM; does not show significant activity for ERα, PR, AR or MR; shows anti-inflammatory efficacy after topical application similar to the classical glucocorticoids, with a better safety profile.Psoriasis Phase 1 Clinical.

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 mapracorat (0.1%) leads to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas.

ZK 245186 | BOL 303242X | BAY-865319

Endocrinology/Hormones

GR

GR

Inflammation/Immunology

Psoriasis

887375-26-0

462.489

C25H26F4N2O2

>98% (HPLC)

DMSO : ≥ 33.6 mg/mL 72.65 mM

CC(C)(C1=CC(F)=CC2=C1OCC2)C[C@@](O)(CNC3=C4C=CC(C)=NC4=CC=C3)C(F)(F)F

(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

(-20℃)

With Ice Pack

≥ 2 years