GSK2033 是LXR的有效拮抗剂,抑制LXRα和LXRβ的pIC50分别为 7 和 7.4。
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GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).
体外活性
GSK2033 dose-dependently inhibits basal transcription in full-length LXRα or full-length LXRβ cotransfection assays (IC50s: 17 nM and 9 nM, respectively). GSK2033 also effectively inhibits the transcription of an ABCA1 driven luciferase reporter dose-dependently (IC50s: 52 nM for LXRα and 10 nM for LXRβ). GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1[2].
体内活性
GSK2033 (one month) treatment, does not have obviously effects on hepatic triglyceride levels. GSK2033 treatment also have no effects on plasma triglyceride levels[2].
Cas No.
1221277-90-2
分子式
C29H28F3NO5S2
分子量
591.66
储存和溶解度
DMSO:30 mg/mL (50.70 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years