(-)-ZK 216348 (C09-1185-994)

(-)-ZK 216348 is the enantiomer of (+)-ZK 216348 ( HY-123352 ). (+)-ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist with an IC 50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC 50 s of 20.4 nAppearance:SolidIC50& Target:IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)In Vitro:In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC 50 of 89 nM and 52 nM, respectively. Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells,In Vivo:ZK 216348 (1-30mg/kg; subcutaneous injection; for 24 hours; NMRI mice and Wistar rats) treatment inhibits ear edema in both mice and rats. A markedly superior side-effect profile is found in ZK 216348 with regard to increases in blood glucose, spleen invBiological Activity:(-)-ZK 216348 is the enantiomer of (+)-ZK 216348 ( HY-123352 ). (+)-ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist with an IC 50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC 50 s of 20.4 n. Specification: 0.98 Molecular Formula: C24H23F3N2O5 Molecular Weight: 476.45