ZK 216348 (C09-1185-927)

ZK 216348 ((+)-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 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effectsIn VitroIn 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, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoZK 216348 (1-30  mg/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 involution, and, to a lesser extent, skin atrophy . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg and 30  mg/kg Administration: Subcutaneous injection; for 24 hours Result: Inhibited ear edema in mice and rats.Form:SolidIC50& Target:IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor). Specification: 0.98 Molecular Formula: C24H23F3N2O5 Molecular Weight: 476.45 PubChem CID: 9805004 Isomeric SMILES: CC1=NOC(=O)C2=C1C=C(C=C2)NC(=O)C(CC(C)(C)C3=CC=CC4=C3OCC4)(C(F)(F)F)O