1. Vitamin D Related
  2. VD/VDR
  3. ZK159222

ZK159222 

Cat. No.: HY-12397
Handling Instructions

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.

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ZK159222 Chemical Structure

ZK159222 Chemical Structure

CAS No. : 156965-15-0

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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].

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].

Molecular Weight

512.72

Formula

C₃₂H₄₈O₅

CAS No.

156965-15-0

SMILES

O=C(C1([[email protected]](O)/C=C/[[email protected]]([[email protected]]2CC[[email protected]@]3([H])/C(CCC[[email protected]]23C)=C/C=C4C([[email protected]@H](O)C[[email protected]](O)C\4)=C)C)CC1)OCCCC

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

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Keywords:

ZK159222ZK 159222ZK-159222VD/VDRVitamin DVitamin D receptorantagonisticactioncoactivatorvitaminDcomplexformationesteranalogueligand-dependentinteractionInhibitorinhibitorinhibit

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ZK159222
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HY-12397
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