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ZK 159222
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。
ZK 159222图片
CAS NO:156965-15-0
包装:500 μg
市场价:7545元

产品介绍
ZK 159222 是 1α,25-(OH)2D3 的 25-羧酸酯类似物,是一种有效的 1α,25-(OH)2D3 受体 (VDR) 拮抗剂。
Cas No.156965-15-0
Canonical SMILESC=C1/C(C[C@@H](O)C[C@@H]1O)=C\C=C2CCC[C@@]3(C)[C@@]/2([H])CC[C@]3([H])[C@H](C)/C=C/[C@@H](O)C4(CC4)C(OCCCC)=O
分子式C32H48O5
分子量512.7
溶解度Chloroform: slightly soluble,Methanol: slightly soluble
储存条件4°C, protect from light, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ZK 159222 is an antagonist of the vitamin D receptor (VDR).1,2It stabilizes the VDR in an antagonistic conformation that prevents interaction with coactivator proteins.3ZK 159222 inhibits VDR-mediated target gene activation when used at concentrations of 300 and 1,000 nM in reporter assays. Preincubation of preadipocytes with ZK 159222 (0.01 and 1 µM) decreases the secretion of IL-1β, IL-6, IL-8, CCL2, and RANTES induced by macrophage-conditioned medium (MacCM).4It also decreases the secretion of these cytokines in preadipocytes prestimulated with MacCM and decreases MacCM-induced phosphorylation of p44/42 and p38 MAPK in preadipocytes.

1.Herdick, M., Steinmeyer, A., and Carlberg, C.Antagonistic action of a 25-carboxylic ester analogue of 1ɑ,25-dihydroxyvitamin D3 is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivatorsJ. Biol. Chem.275(22)16506-16512(2000) 2.Herdick, M., Steinmeyer, A., and Carlberg, C.Carboxylic ester antagonists of 1ɑ,25-dihydroxyvitamin D3 show cell-specific actionsChem. Biol.7(11)885-894(2000) 3.Bury, Y., Steinmeyer, A., and Carlberg, C.Structure activity relationship of carboxylic ester antagonists of the vitamin D3 receptorMol. Pharmacol.58(5)1067-1074(2000) 4.Zhu, J., and Wilding, J.P.H.The 1α,25(OH)2D3 analogs ZK159222 and ZK191784 show anti-inflammatory properties in macrophage-induced preadipocytes via modulating the NF-κB and MAPK signalingDiabetes Metab. Syndr. Obes.131715-1724(2020)