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。

ZK168281 is a 25-carboxylic ester 1α,25(OH) 2 D 3 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.

Solid

Kd: 0.1 nM (VDR)

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

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Lempi?inen H, et al. Antagonist- and inverse agonist-driven interactions of the vitamin D receptor and the constitutive androstane receptor with corepressor protein. Mol Endocrinol. 2005 Sep;19(9):2258-72.

In Vitro: DMSO : 100 mg/mL (195.81 mM; Need ultrasonic)配制储备液