SML1617
GSK2033
≥98% (HPLC), nuclear receptor liver-X-receptor (LXR) antagonist, powder
别名:
2,4,6-三甲基-N-[[3′-(甲基磺酰基)[1,1′-联苯]-4-基]甲基]-N-[[5-(三氟甲基)-2-呋喃基]甲基]苯磺酰胺
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关于此项目
经验公式（希尔记法）:
C29H28F3NO5S2
化学文摘社编号:
分子量:
591.66
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
GSK2033, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 3 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
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
Biochem/physiol Actions
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。
LXR拮抗剂
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Separating the Anti-Inflammatory and Diabetogenic Effects of Glucocorticoids Through LXRβ Antagonism.
Patel R, et al.
Endocrinology, 158(4), 1034-1047 (2017)
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)
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1617-25MG | 04061832955513 |
| SML1617-5MG | 04061832955520 |