Formulation: A solid
Formal Name: 1-[(1R,2E,4R)-4-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylenecyclohexylidene]ethylidene]octahydro-7a-methyl-1H-inden-1-yl]-1-hydroxy-2-penten-1-yl]-cyclopropanecarboxylic acid, butyl ester
Purity: ≥95%
Formula Markup: C32H48O5
Formula Weight: 512,7
Shelf life (days): 730
CAS Number: 156965-15-0
Notes: ZK 159222 is an antagonist of the vitamin D receptor (VDR).{52664,52665} It stabilizes the VDR in an antagonistic conformation that prevents interaction with coactivator proteins.{52666} ZK 159222 inhibits VDR-mediated target gene activation when used at concentrations of 300 and 1,000 nM in reporter assays. Preincubation of preadipocytes with ZK 159222 (0.01 and 1 µM) decreases the secretion of IL-1β, IL-6, IL-8, CCL2, and RANTES induced by macrophage-conditioned medium (MacCM).{52667} It also decreases the secretion of these cytokines in preadipocytes prestimulated with MacCM and decreases MacCM-induced phosphorylation of p44/42 and p38 MAPK in preadipocytes.
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