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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
4°C, protect from light, stored under nitrogen
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
186371-96-0
- 规格:
1 mg
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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,Kd 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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