ZK-216348

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

ZK-216348 是一种有效的、选择性的解离糖皮质激素受体激动剂，pIC50 为 7.7。

ZK-216348 is a potent, selective, dissociated glucocorticoid receptor agonist with pIC50 of 7.7, shows selectivity over other nuclear hormone receptors.

In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC50 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.

ZK 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. 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.

ZK216348

Endocrinology/Hormones

GR

GR

——

——

669073-68-1

476.45

C24H23F3N2O5

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (419.77 mM)

CC(C)(C1=CC=CC2=C1OCC2)CC(C(F)(F)F)(O)C(NC3=CC=C(C(ON=C4C)=O)C4=C3)=O

4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide

(-20℃)

With Ice Pack

≥ 2 years