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ZK168281
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。
ZK168281图片
CAS NO:186371-96-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
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。
生物活性

ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3analog and a pureVDRantagonist with aKdvalue of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor[1].

IC50& Target

Kd: 0.1 nM (VDR)[1]

体外研究
(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[1].

分子量

510.70

性状

Solid

Formula

C32H46O5

CAS 号

186371-96-0

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)

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 mg5 mg10 mg
1 mM1.9581 mL9.7905 mL19.5810 mL
5 mM0.3916 mL1.9581 mL3.9162 mL
10 mM0.1958 mL0.9790 mL1.9581 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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。