1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. ZK 216348

ZK 216348 (Synonyms: (+)-ZK 216348)

Cat. No.: HY-123352
Handling Instructions

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.

For research use only. We do not sell to patients.

ZK 216348 Chemical Structure

ZK 216348 Chemical Structure

CAS No. : 669073-68-1

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Description

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects[1][2].

IC50 & Target

IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)[1]

In Vitro

In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC50 of 89 nM and 52 nM, respectively[1].
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[2].

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[1].

Animal Model: NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil[1]
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.
Molecular Weight

476.45

Formula

C₂₄H₂₃F₃N₂O₅

CAS No.

669073-68-1

SMILES

O=C1C2=CC=C(C=C2C(C)=NO1)NC(C(C(F)(F)F)(O)CC(C)(C3=C4C(CCO4)=CC=C3)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ZK 216348(+)-ZK 216348ZK216348ZK-216348Glucocorticoid ReceptorNonsteroidalantiinflammatorytransactivation-mediatedside effectsprogesteronemineralocorticoidInhibitorinhibitorinhibit

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ZK 216348
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HY-123352
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