ZK168281|cas:186371-96-0|西域试剂

ZK168281,98.43%

产品编号：Bellancom-12407| CAS NO：186371-96-0| 分子式：C₃₂H₄₆O₅| 分子量：510.70

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-12407		￥13500.00	杭州北京（现货）

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ZK168281

产品介绍

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。

生物活性

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

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (195.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9581 mL	9.7905 mL	19.5810 mL
5 mM	0.3916 mL	1.9581 mL	3.9162 mL
10 mM	0.1958 mL	0.9790 mL	1.9581 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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)

参考文献