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CD 3254
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。
CD 3254图片
CAS NO:196961-43-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
CD 3254 是一种有效的选择性维甲酸 X 受体 (RXR) 激动剂。
Cas No.196961-43-0
化学名(E)-3-(4-hydroxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl)acrylic acid
Canonical SMILESOC1=CC=C(/C=C/C(O)=O)C=C1C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2
分子式C24H28O3
分子量364.48
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2)(1:8): 0.11 mg/ml,Ethanol: 20 mg/ml
储存条件Store at -20°C
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

CD3254 is a potent and selective agonist of Retinoid X receptors (RXRα).

Retinoid X receptors (RXRs) are nuclear receptors that act as ligand-dependent transcription factors and function as the homodimer or as heterodimers with other nuclear receptors, such as retinoic acid receptors (RARs), peroxisome proliferator-activated receptors (PPARs), or liver X receptors (LXRs). RXR plays essential roles in the regulation of glucose metabolism, lipid metabolism and immune response. Retinoid X receptors (RXRs) contains three family members including RARα, RARβ or RARγ receptors. RXRα belongs to the NR2B nuclear receptor family and primarily expressed in the liver, intestines, kidneys, and epidermis.

CD3254 and its’ analogue bexarotene have been reported as a treatment for cutaneous T-cell lymphoma (CTCL), despite the fact that treatment with CD3254 can evoke reactions by disturbing other RXR-heterodimer receptor pathways. Of the seven displayed novel exacerbates, all analogs animate RXR-controlled translation in mammalian 2 hybrid and RXRE-interceded tests, have equivalent or hoisted natural action in view of EC50 profiles, and hold comparative or enhanced apoptotic movement in CTCL assays contrasted with CD3254. Every single novel compound show selectivity for RXR and insignificant hybrid onto the retinoic corrosive receptor (RAR) contrasted with all-trans-retinoic corrosive, with select analogs likewise decreasing hindrance of other RXR-subordinate pathways (e.g., VDR-RXR) [1].

In vivo, CD3254 induced the phenotypes of malformations after 5 days exposure at low concentration (20 μg/l) to those after the 1st d exposure at high concentrations (50 and 100 μg/L) [2].

References:
Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid (CD3254).  J Med Chem. 2013 Nov 14;56(21):8432-54. doi: 10.1021/jm4008517. Epub 2013 Nov 1.
Divergent teratogenicity of agonists of retinoid X receptors in embryos of zebrafish (Danio rerio).  Ecotoxicology. 2012 Jul;21(5):1465-75. doi: 10.1007/s10646-012-0900-9. Epub 2012 Apr 10.