ZK168281,186371-96-0

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ZK168281

CAS No. : 186371-96-0

MCE 国际站：ZK168281

产品活性：ZK168281 是一种 1α,25(OH)₂D₃ 类似物，也是一种纯 VDR 拮抗剂，K_d 值为 0.1 nM。ZK168281 是其受体 CoA 相互作用的有效抑制剂。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：VD/VDR

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.

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