中文名 | GW3965 hydrochloride |
英文名 | 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride |
别名 | 3-氧代异吲啉-5-甲腈 化合物GW3965 HCL 3-[3-[(2-氯-3-三氟甲基苄基)(2,2-二苯基乙基)氨基]丙氧基]苯乙酸盐酸盐 2-[3-[3-[[2-氯-3-(三氟甲基)苄基](2,2-二苯基乙基)氨基]丙氧基]苯基]乙酸盐酸盐 |
英文别名 | GW3965 HCl GW3965 HCl Salt GW3965 hydrochloride GW 3965 HYDROCHLORIDE 3-[3-[n-(2-chloro-3-trifluoroMethylbenzyl)-(2,2-di… 3-[3-[n-(2-chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyloxy]phenylacetic acid hydrochloride 2-[3-[3-[[2-Chloro-3-(trifluoromethyl)benzyl](2,2-diphenylethyl)amino]propoxy]phenyl]acetic acid hydrochloride 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride 3-[3-[[[2-Chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]benzeneacetic acid hydrochloride Benzeneacetic acid, 3-[3-[[[2-chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]-, hydrochloride |
CAS | 405911-17-3 |
化学式 | C33H31ClF3NO3.HCl |
InChIKey | NMPUWJFHNOUNQU-UHFFFAOYSA-N |
溶解度 | DMSO: ≥ 20 mg/mL |
存储条件 | -20°C |
外观 | 粉末 |
颜色 | white |
MDL号 | MFCD08276920 |
靶点 | hLXRα;hLXRβ;LXRα/SRC1 LiSA |
体外研究 | GW3965使类固醇受体共激活因子1聚集到LXRα,在无细胞配体检测试验中,EC50 为125 nM。 GW3965对hLXRα 和 hLXRβ表现出有效的拮抗活性,在细胞试验中EC50分别为190 nM 和30 nM。此外,GW3965也对其他核受体表现出优良的选择性。在人胰岛中,GW3965 (1 μM)降低选定促炎性细胞因子,包括IL-8,单核细胞趋化蛋白-1和组织因子的表达。 |
体内研究 | 在小鼠体内,GW3965在10 mg/kg剂量下使ABCA1表达上调8倍,并使循环水平提高30%,C max为12.7 μg/mL ,t 1/2为2小时。 在LDLR−/−和apoE−/−小鼠体内,GW3965 (10mg/kg)诱导ABCA1 和ABCG1表达,并表现出有效的抗动脉粥样硬化活性。在雄性sprague-dawley大鼠体内,GW3965降低Ang II介导的血压增加,并减少血管Ang II受体基因表达。在恶性胶质瘤小鼠模型中,GW3965导致LDLR降解,增加ABCA1胆固醇外排转运体的表达,从而有效促进肿瘤细胞死亡。 |
危险品标志 | Xn - 有害物品 |
风险术语 | R22 - 吞食有害。 R41 - 对眼睛有严重伤害。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S39 - 戴护目镜或面具。 |
WGK Germany | 3 |
参考资料 展开查看 | 1: Wang R, Li R, Wen Q, Peng K, Tan X, Chen Z. [Expression of LXR-β in human gastric cancer tissue and the effect of GW3965 on the proliferation of gastric cancer cell line SGC-7901]. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2016 Feb 28;41(2):127-33. doi: 10.11817/j.issn.1672-7347.2016.02.003. Chinese. PubMed PMID: 26932209. 2: Nunomura S, Okayama Y, Matsumoto K, Hashimoto N, Endo-Umeda K, Terui T, Makishima M, Ra C. Activation of LXRs using the synthetic agonist GW3965 represses the production of pro-inflammatory cytokines by murine mast cells. Allergol Int. 2015 Sep;64 Suppl:S11-7. doi: 10.1016/j.alit.2015.03.001. Epub 2015 Mar 31. PubMed PMID: 26344074. 3: Archer A, Stolarczyk E, Doria ML, Helguero L, Domingues R, Howard JK, Mode A, Korach-André M, Gustafsson JÅ. LXR activation by GW3965 alters fat tissue distribution and adipose tissue inflammation in ob/ob female mice. J Lipid Res. 2013 May;54(5):1300-11. doi: 10.1194/jlr.M033977. Epub 2013 Feb 27. PubMed PMID: 23446231; PubMed Central PMCID: PMC3622325. 4: Namjoshi DR, Martin G, Donkin J, Wilkinson A, Stukas S, Fan J, Carr M, Tabarestani S, Wuerth K, Hancock RE, Wellington CL. The liver X receptor agonist GW3965 improves recovery from mild repetitive traumatic brain injury in mice partly through apolipoprotein E. PLoS One. 2013;8(1):e53529. doi: 10.1371/journal.pone.0053529. Epub 2013 Jan 17. PubMed PMID: 23349715; PubMed Central PMCID: PMC3547922. 5: Cui X, Chopp M, Zacharek A, Cui Y, Roberts C, Chen J. The neurorestorative benefit of |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.617 ml | 8.084 ml | 16.168 ml |
5 mM | 0.323 ml | 1.617 ml | 3.234 ml |
10 mM | 0.162 ml | 0.808 ml | 1.617 ml |
5 mM | 0.032 ml | 0.162 ml | 0.323 ml |
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