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 effects 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, 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 Vivo 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 . 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:Solid IC50& Target:IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)
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ZK 216348
CAS number：669073-68-1 molecular formula：C24H23F3N2O5
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| Chinese alias | 售卖处 | ||
| English alias | (-)-ZK 216348 | GTPL8643 | HY-123352A | (+)-Zk 216348 | ZK 216348, (+)- | 4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide | E99033 | (+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydro | ||
| CAS number | 669073-68-1 | molecular formula | C24H23F3N2O5 |
| molecular weight | 476.45 g/mol | Exact mass | ≥98% |
| PSA | 97.200 Ų | logp | 4.3 |
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