质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 3 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
CS(C1=CC=CC(C2=CC=C(CN(S(C3=C(C)C=C(C)C=C3C)(=O)=O)CC4=CC=C(C(F)(F)F)O4)C=C2)=C1)(=O)=O
InChI
1S/C29H28F3NO5S2/c1-19-14-20(2)28(21(3)15-19)40(36,37)33(18-25-12-13-27(38-25)29(30,31)32)17-22-8-10-23(11-9-22)24-6-5-7-26(16-24)39(4,34)35/h5-16H,17-18H2,1-4H3
InChI key
PSOXOVKYGWBTPB-UHFFFAOYSA-N
生化/生理作用
GSK2033具有抑制GC（糖皮质激素）刺激的糖异生基因表达的能力，而不会改变免疫反应性GR（GC受体）靶基因。它有助于靶向可以改变肝基因表达的几种核受体。
GSK2033是核受体肝X受体(LXR)的拮抗剂，LXRα的pIC50值为7.0，LXRβ的pIC50值为7.4。用GSK2033处理鼠CD41 T细胞可增强细胞增殖和Th1/Th2/Th17分化。在另一项研究中，通过与GSK2033预孵育，完全消除了共轭亚油酸（CLA）诱导的外排蛋白ATP结合盒转运蛋白A1（ABCA1）的表达，表明CLA介导的ABCA-1表达调控是LXR依赖性的。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver disease.
Griffett K and Burris TP
Biochemical and Biophysical Research Communications, 479(3), 424-428 (2016)
Separating the Anti-Inflammatory and Diabetogenic Effects of Glucocorticoids Through LXRβ Antagonism.
Patel R, et al.
Endocrinology, 158(4), 1034-1047 (2017)
Lili Chen et al.
Journal of neurochemistry, 154(2), 205-217 (2019-10-12)
Cerebral ischemia (CI) leads to cognitive dysfunction due to the loss of hippocampal neurons. Liver X receptors (LXRs), including the LXRα and LXRβ isoforms, are critical for neurogenesis, synaptic plasticity, neurodegeneration, and cholesterol metabolism. However, the potential role of LXRs
Louise Ménégaut et al.
Cell reports, 31(7), 107665-107665 (2020-05-21)
Low-grade inflammation is constitutive of atherosclerosis, and anti-inflammatory therapy inhibiting interleukin-1β (IL-1β) reduces the rate of cardiovascular events. While cholesterol accumulation in atheroma plaque and macrophages is a major driver of the inflammatory process, the role of the LXR cholesterol
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