ZK159222

Names

[ Name ]:
ZK159222

[Synonym ]:
Butyl (1S,3R,5Z,7E,22E,24R)-1,3,24-trihydroxy-26,27-cyclo-9,10-secocholesta-5,7,10,22-tetraene-25-carboxylate
ZK159222
Cyclopropanecarboxylic acid, 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]-, butyl ester

Biological Activity

[Description]:

ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) agonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character[1].

[Related Catalog]:

Signaling Pathways >> Vitamin D Related >> VD/VDR

Research Areas >> Endocrinology

[In Vitro]

ZK159222, displayed the profile of a weak VDR agonists that requires an approximate 7-fold higher concentration than of the natural hormone 1α,25-(OH)2D3 to stabilize VDR-RXR heterodimer complex formation on a DR3-type VDRE. ZK159222 was found to belong to the category of 1α,25-(OH)2D3 analogues that stabilize an additional third functional VDR conformation, which has also been described for some agonistic 20-epi analogues. The remaining reporter gene activity that was obtained by a combined treatment of 10 nM 1α,25-(OH)2D3 with 1 μM ZK159222 is close to the partial agonistic activity of 1 μM ZK159222[1].

[References]

[1]. Herdick M, et al. Antagonistic action of a 25-carboxylic ester analogue of 1alpha, 25-dihydroxyvitamin D3 is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. J Biol Chem. 2000 Jun 2;275(22):16506-12.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
646.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₂H₄₈O₅

[ Molecular Weight ]:
512.721

[ Flash Point ]:
201.1±25.0 °C

[ Exact Mass ]:
512.350159

[ LogP ]:
6.46

[ Vapour Pressure ]:
0.0±4.4 mmHg at 25°C

[ Index of Refraction ]:
1.568

Related Compounds

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