1. Vitamin D Related
  2. VD/VDR
  3. ZK168281

ZK168281 

Cat. No.: HY-12407
Handling Instructions

ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.

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

ZK168281 Chemical Structure

ZK168281 Chemical Structure

CAS No. : 186371-96-0

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Description

ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor[1].

IC50 & Target

Kd: 0.1 nM (VDR)[1]

In Vitro

ZK168281 resembles more the mouse constitutive androstane receptor (CAR) inverse agonist Androstanol in its ability to recruit corepressor (CoR) proteins. A salt bridge between the CoR and a conserved lysine in helix 4 of the nuclear receptor (NR) is central to this interaction, but also helix 12 was stabilized by direct contacts with residues of the CoR. Fixation of helix 12 in the antagonistic/inverse agonistic conformation prevents an energetically unfavorable free floatation of the C terminus[1].

Molecular Weight

510.70

Formula

C₃₂H₄₆O₅

CAS No.

186371-96-0

SMILES

O=C(OCC)/C=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

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:

ZK168281ZK 168281ZK-168281VD/VDRVitamin DVitamin D receptorVDRCoAinteractionNR25-carboxylicesterInhibitorinhibitorinhibit

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HY-12407
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