ZK 216348 is a non-steroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to progesterone receptors and mineralocorticoid receptors with IC₅₀ values of 20.4 nM and 79.9 nM, respectively, and may be useful for studying inflammatory bowel disease (IBD).

Mineralocorticoid receptor:79.9 nM, Progesterone receptor:20.4 nM, Glucocorticoid receptor:20.3 nM

In PBMCs, ZK 216348 can inhibit the production of TNF-α and IL-12, with IC50 values of 89 nM and 52 nM, respectively [1].
ZK 216348 significantly suppresses TNF-α-induced IL-8 expression levels in homo sapiens colorectal adenocarcinoma cells (Caco-2) [2].

Following administration of ZK 216348 (1-30 mg/kg, subcutaneous injection, for 24 hours) to NMRI mice and Wistar rats, ear edema symptoms in both animal models were significantly suppressed. The study found that compared to the control drug, ZK 216348 demonstrated distinct advantages in terms of adverse reactions, specifically manifested in its inhibitory effects on blood glucose elevation and spleen atrophy, while also exhibiting a relatively milder impact on skin atrophy [1].