EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73102_C
视黄酸通路激活剂；激活视黄酸受体（RAR）
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总览
EC23是一种视黄酸受体（RAR）激动剂，具有广谱RAR活性（EC₅₀：RARα 41 nM, RARβ 0.5 nM, RARγ 0.4 nM），而对视黄酸受体(RXR；EC₅₀> 10μM；Gambone等人)无显著活性。它是一种对光稳定的全反式视黄酸（ATRA）的合成类似物（Christie 等，2008）。此外，EC23 还能弱激活芳烃受体（Gambone 等人）。
分化
·诱导人多能干细胞向神经分化，类似于ATRA (Christie 等人，2010；Clemens等人)。
·诱导人胎儿神经祖细胞系ReNcell 197VM的神经元分化（Christie 等人. 2010）。
细胞类型
神经细胞，PSC衍生，神经干/祖细胞，神经元，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化
研究领域
神经科学，干细胞生物学
CAS 编号
104561-41-3
化学式
C₂₃H₂₄O₂
纯度
≥98%
通路
视黄醇类
靶点
RAR
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
本产品专为以下研究领域设计，适用于工作流程中的高亮阶段。探索这些工作流程，了解更多我们为各研究领域提供的其他配套产品。
相关材料与文献
技术资料 (3)
文献 (4)
Unique property of some synthetic retinoids: activation of the aryl hydrocarbon receptor pathway.
Molecular pharmacology 2002
Abstract
Potential pharmacological applications in the areas of oncology,dermatology,diabetes,and atherosclerosis of synthetic analogs of retinoic acid that target a specific nuclear receptor and/or biological response have generated great interest in the development of new retinoid and rexinoid drugs. The pan-retinoic acid receptor antagonist AGN 193109 has been previously reported to elevate CYP1A1 levels,implicating the aryl hydrocarbon receptor (AhR) as an additional target for this retinoid. AhR is a cytosolic ligand-dependent transcription factor that,in conjunction with the AhR nuclear translocator (Arnt),binds to dioxin response elements (DREs) located in the promoter region of target genes,such as CYP1A1,and induces their transcription. The purpose of these studies was to determine whether additional synthetic retinoids were capable of elevating CYP1A1 levels and to examine the mechanism of this increase in CYP1A. Two additional retinoids,AGN 190730 and AGN 192837,were found to be potent inducers of DRE-driven transcriptional activity; AGN 190730 was the most potent. Moreover,electrophoretic mobility-shift assays demonstrate that AGN 190730 can transform AhR into its active DNA recognition form. In addition,trypsin digestion of AGN 190730-treated AhR reveals a conformational change in the protein similar to the conformational change of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-bound AhR. Finally,competitive binding studies demonstrate that AGN 190730 can inhibit the binding of TCDD to AhR. The sum of the data demonstrates that some synthetic retinoids in addition to activating the retinoic acid receptor/retinoid X receptor pathway are capable of binding to AhR and activating the AhR/Arnt pathway.
Synthesis and evaluation of synthetic retinoid derivatives as inducers of stem cell differentiation.
Organic & biomolecular chemistry 2008 OCT
Abstract
All-trans-retinoic acid (ATRA) and its associated analogues are important mediators of cell differentiation and function during the development of the nervous system. It is well known that ATRA can induce the differentiation of neural tissues from human pluripotent stem cells. However,it is not always appreciated that ATRA is highly susceptible to isomerisation when in solution,which can influence the effective concentration of ATRA and subsequently its biological activity. To address this source of variability,synthetic retinoid analogues have been designed and synthesised that retain stability during use and maintain biological function in comparison to ATRA. It is also shown that subtle modifications to the structure of the synthetic retinoid compound impacts significantly on biological activity,as when exposed to cultured human pluripotent stem cells,synthetic retinoid 4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-ylethynyl)benzoic acid,4a (para-isomer),induces neural differentiation similarly to ATRA. In contrast,stem cells exposed to synthetic retinoid 3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-ylethynyl)benzoic acid,4b (meta-isomer),produce very few neurons and large numbers of epithelial-like cells. This type of structure-activity-relationship information for such synthetic retinoid compounds will further the ability to design more targeted systems capable of mediating robust and reproducible tissue differentiation.
Retinoid supplementation of differentiating human neural progenitors and embryonic stem cells leads to enhanced neurogenesis in vitro.
Journal of neuroscience methods 2010 NOV
Abstract
Retinoids are important molecules involved in the development and homeostasis of the nervous system. As such,various retinoid derivatives are often found in culture media and supplement formulations to support the growth and maintenance of neural cells. However,all-trans-retinoic acid (ATRA) and its associated derivatives are light sensitive and are highly susceptible to isomerisation. This can lead to variability in retinoid concentrations and the nature of the retinoid species present in culture solutions which in turn can influence biological activity and introduce inconsistency. We have previously described the development of the synthetic retinoid derivative,EC23,as a chemically and light stable alternative that does not degrade and has biological activity similar to ATRA. In this study we demonstrate that the addition of exogenous retinoid can significantly enhance neuronal differentiation of both human neuroprogenitor and human embryonic stem cells. In the former,both ATRA and EC23 induced increased maturation and stabilisation of the axonal cytoskeleton. However,EC23 was particularly potent at lower nanomolar concentrations resulting in significantly greater neurogenesis than ATRA. In ES cells enhanced motor neuron marker expression was also detected in response to both retinoids when incorporated into an established protocol for neuronal differentiation. We propose that synthetic retinoid EC23 represents a valuable addition to the formulation of new and existing culture supplements to enhance neuronal differentiation whilst enabling improved consistency.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 104561-41-3 |
| Chemical Formula | C₂₃H₂₄O₂ |
| 纯度 | ≥ 98% |
| Target | RAR |
| Pathway | Retinoid |
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