中文名 | UVI 3003 |
英文名 | UVI 3003 |
别名 | 化合物UVI 3003 3-[4-羟基-3-[5,6,7,8-四氢-5,5,8,8-四甲基-3-(戊基氧基)-2-萘]苯基]-2-丙酸 |
英文别名 | UVI3003 UVI-3003 UVI 3003 3-[4-Hydroxy-3-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-(pentyloxy)-2-naphthalenyl]phenyl]-2-propenoicacid 2-Propenoic acid, 3-[4-hydroxy-3-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-(pentyloxy)-2-naphthalenyl]phenyl]- |
CAS | 847239-17-2 |
化学式 | C28H36O4 |
分子量 | 436.58 |
溶解度 | 溶于DMSO |
存储条件 | Inert atmosphere,Store in freezer, under -20°C |
靶点 | Xenopus RXRα, in Cos7 cells Human RXRα, in Cos7 cells |
体外研究 | UVI3003 inhibits the activity of xenopus and human RXRα, with IC 50 s of 0.22 and 0.24 μM, respectively. UVI3003 fully activates xPPARγ with an EC 50 of 12.6 μM, and is almost completely inactive on hPPARγ and mPPARγ. UVI 3003 (10 μM) does not change the proliferation rate of extraocular muscles (EOM)-derived or LEG-derived EECD34 cells. UVI 3003 causes a 65.4% difference in EECD34 cell fusion and desmin expression. |
参考资料 展开查看 | 1: Zhu J, Janesick A, Wu L, Hu L, Tang W, Blumberg B, Shi H. The unexpected teratogenicity of RXR antagonist UVI3003 via activation of PPARγ in Xenopus tropicalis. Toxicol Appl Pharmacol. 2017 Jan 1;314:91-97. doi: 10.1016/j.taap.2016.11.014. Epub 2016 Nov 25. PubMed PMID: 27894914; PubMed Central PMCID: PMC5183475. 2: Mihály J, Gericke J, Lucas R, de Lera AR, Alvarez S, Törőcsik D, Rühl R. TSLP expression in the skin is mediated via RARγ-RXR pathways. Immunobiology. 2016 Feb;221(2):161-5. doi: 10.1016/j.imbio.2015.09.013. Epub 2015 Sep 10. PubMed PMID: 26531761. 3: Zheng L, Yu J, Shi H, Xia L, Xin Q, Zhang Q, Zhao H, Luo J, Jin W, Li D, Zhou J. Quantitative toxicoproteomic analysis of zebrafish embryos exposed to a retinoid X receptor antagonist UVI3003. J Appl Toxicol. 2015 Sep;35(9):1049-57. doi: 10.1002/jat.3099. Epub 2015 Jan 11. PubMed PMID: 25581642. 4: Sun J, Narayanasamy S, Curley RW Jr, Harrison EH. β-Apo-13-carotenone regulates retinoid X receptor transcriptional activity through tetramerization of the receptor. J Biol Chem. 2014 Nov 28;289(48):33118-24. doi: 10.1074/jbc.M114.610501. Epub 2014 Oct 16. PubMed PMID: 25324544; PubMed Central PMCID: PMC4246072. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.291 ml | 11.453 ml | 22.905 ml |
5 mM | 0.458 ml | 2.291 ml | 4.581 ml |
10 mM | 0.229 ml | 1.145 ml | 2.291 ml |
5 mM | 0.046 ml | 0.229 ml | 0.458 ml |
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