Methylprednisolone aceponate

Methylprednisolone aceponate (ZK 91588) is a glucocorticoid and anti-inflammatory agent with weak systemic effects. Methylprednisolone aceponate is a selective glucocorticoid receptor Ligand.Methylprednisolone aceponate can be used for research of eczema and other inflammatory skin disorders.

Methylprednisolone aceponate inhibits collagenase promoter activity (in HeLa cells), LPS-induced IL-12p40 secretion (in human PBMCs) and phytohemagglutinin-induced IFN-γ secretion (in human PBMCs) with IC₅₀s of 9.3, 16.8, 15.2 nM^[3].
Methylprednisolone aceponate induces MMTV promoter and TAT activities with EC₅₀s of 21.8 and 20.5 nM respectively^[3].

Methylprednisolone aceponate (topically applied, 50 μL,，Coroton oil-induced Evan blue edema) shows anti-inflammatory effect with an IC₅₀ of 0.0015%, with low systemic side effect^[1].
Methylprednisolone aceponate (0.0001%-0.1%, topically applied) inhibits oedema formation with ED₅₀ of 0.002% in irritant contact dermatitis in mice and rat^[3].

References:
[1]. Ruzicka T. Methylprednisolone aceponate in eczema and other inflammatory skin disorders -- a clinical update. Int J Clin Pract. 2006 Jan;60(1):85-92.
[2]. H.J. Zentel, et al. Preclinical evaluation of a new topical corticosteroid methylprednisolone aceponate. 1994. 3 (s1), S32-S38.
[3]. Schäcke H, et al. Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases. Br J Pharmacol. 2009 Oct;158(4):1088-103.