產(chǎn)品屬性：
產(chǎn)品名稱 | ZK 159222 |
規(guī)格 | 500 μg |
貨號 | EY-01Y16390 |
Cas No.: 156965-15-0
別名: N/A
化學(xué)名: N/A
分子式: C32H48O5
分子量: 512.7
溶解度: Chloroform: slightly soluble,Methanol: slightly soluble
儲存條件: 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
產(chǎn)品描述：
ZK 159222 is an antagonist of the vitamin D receptor (VDR).1,2 It stabilizes the VDR in an antagonistic conformation that prevents interaction with coactivator proteins.3 ZK 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).4 It 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)
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