2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. GSK-9772

GSK-9772 是一种 N-苯基叔胺类 (NPTAs) 的 Liver X Receptor (LXR) 调节剂，对 LXR β 配体有高亲和力 (IC50=30 nM)。GSK-9772 具有抗炎活性，通过与 LXR 结合，特别是通过与受体的转录抑制功能相关联的区域相互作用，来实现对促炎基因表达的抑制。GSK-9772 可用于炎症和神经退行性疾病的研究。

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GSK-9772 Chemical Structure

GSK-9772 Chemical Structure

CAS No. : 928035-84-1

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GSK-9772 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-9772 is a Liver X Receptor (LXR) modulator of the N-phenyl tertiary amine class (NPTAs) with high affinity for LXR β ligand (IC50=30 nM). GSK-9772 has anti-inflammatory activity by binding to LXR, specifically by interacting with the region associated with the transcriptional repression function of the receptor, thereby inhibiting the expression of pro-inflammatory genes. GSK-9772 can be used in the study of inflammatory and neurodegenerative diseases[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
THP-1 IC50
> 10 μM
Compound: 5
Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA
Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA
[PMID: 22873709]
THP-1 IC50
15 nM
Compound: 20, GSK-9772
Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA
Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA
[PMID: 18800767]
分子量

490.27

Formula

C20H19Cl2F6NO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSK-9772 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-9772928035-84-1GSK9772GSK 9772LXRLiver X receptorModulatorsAnti-inflammatory activityTranscriptional repressionNeurodegenerative diseasesInhibitorinhibitorinhibit

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