2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. GW409544

GW409544 是一种双重过氧化物酶体增殖物激活受体 α/γ (PPARα/PPARγ) 激动剂，其 EC50 值分别为 2.3 nM 和 0.28 nM。GW409544 可与 PPARα 和 PPARγ 配体结合域中的残基形成氢键，稳定 AF2 螺旋以形成能够募集辅激活因子肽的电荷钳，并激活受体的转录活性。GW409544 有助于调节葡萄糖、脂质和胆固醇代谢。GW409544 可用于代谢性和心血管疾病的研究。

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GW409544

GW409544 Chemical Structure

CAS No. : 258345-41-4

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GW409544 相关抗体

Top Publications Citing Use of Products

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GW409544 is a dual peroxisome proliferator-activated receptor alpha/gamma (PPARα/PPARγ) agonist with EC50 values of 2.3 and 0.28 nM. GW409544 forms hydrogen bonds with residues in PPARα and PPARγ ligand binding domains, stabilizes the AF2 helix to create a charge clamp that recruits coactivator peptides, and activates receptor transcriptional activity. GW409544 contributes to regulation of glucose, lipid, and cholesterol metabolism. GW409544 can be used for the research of metabolic and cardiovascular disease[1][2].

IC50 & Target[1]

PPARα

2.3 nM (EC50)

PPAR-γ

0.28 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.0027 μM
Compound: GW-409544
Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay
Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay
[PMID: 20299214]
HEK293 EC50
0.01 μM
Compound: GW-409544
Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay
Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay
[PMID: 20299214]
体外研究
(In Vitro)

GW409544 是野生型人源 PPARα (EC50 = 2.3 ± 0.5 nM) 和野生型人源 PPARγ (EC50 = 0.28 ± 0.06 nM) 的强效双重完全激动剂，在浓度高达 10 μM 时对野生型人源 PPARδ 无活性，且对 PPARαY314H 和 PPARγH323Y 保持相近的效力[1]。
GW409544 可通过特异性氢键和疏水相互作用，以能稳定受体激活态的构象结合人源 PPARγ LBD，这一点在分辨率为 2.3-Å 的 PPARγ/RXRα 异二聚体复合物 X 射线晶体结构中得到了直观呈现[1]。
GW409544 可稳定结合并维持人源 PPARα 和人源 PPARγ 的 AF2 螺旋激活结构域[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GW409544 相关抗体:
分子量

510.58

Formula

C31H30N2O5
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

GW409544 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

GW409544258345-41-4GW 409544GW-409544PPARPeroxisome proliferator-activated receptorsAF2 helixlipid metabolismligand binding domainsglucose metabolismperoxisome proliferator-activated receptor alpha (PPARα)coactivator peptidestype-2 diabetesperoxisome proliferator-activated receptor delta (PPARδ)peroxisome proliferator-activated receptor gamma (PPARγ)wild-type human PPARαInhibitorinhibitorinhibit

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HY-121448
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