ZK168281 |
Catalog No.GC63266 |
ZK168281 est un analogue de l'ester 25-carboxylique 1α,25(OH)2D3 et un antagoniste VDR pur avec une valeur Kd de 0,1 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 186371-96-0
Sample solution is provided at 25 µL, 10mM.
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].
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].
[1]. LempiÄinen H, et al. Antagonist- and inverse agonist-driven interactions of the vitamin D receptor and the constitutive androstane receptor with corepressor protein. Mol Endocrinol. 2005 Sep;19(9):2258-72.
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