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ZK159222
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZK159222图片
CAS NO:156965-15-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
ZK159222 是 1α,25-(OH)2D3 的类似物,是有效的 1α,25-(OH)2D3 受体(VDR)拮抗剂。ZK159222 拮抗作用的机制是由配体诱导的维生素 D 受体与辅助激活剂的相互作用缺乏所介导的。ZK159222 具有部分激动性。
生物活性

ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent1α,25-(OH)2D3 receptor (VDR) antagonist. 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].

体外研究
(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].

分子量

512.72

性状

Solid

Formula

C32H48O5

CAS 号

156965-15-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)