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G5045

Sigma-Aldrich

GW6471

≥98% (HPLC), powder, PPARα antagonist

别名:

N-((2S)-2-(((1Z)-1-甲基-3-氧代-3-(4-(三氟甲基)苯基)丙-1-烯基)胺基)-3-(4-(2-(5-甲基-2-苯基-1,3-恶唑-4-基)乙氧基)苯基)丙基)丙酰胺

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About This Item

经验公式（希尔记法）:
C35H36F3N3O4
CAS号:
880635-03-0
分子量:
619.67
MDL號碼:
MFCD07784503
分類程式碼代碼:
12352200
PubChem物質ID:
24724489
NACRES:
NA.77
价格与库存信息目前不能提供

产品名称

GW6471, ≥98% (HPLC)

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: 5 mg/mL, clear (warmed)

起源

GlaxoSmithKline

儲存溫度

2-8°C

SMILES 字串

CCC(=O)NC[C@H](Cc1ccc(OCCc2nc(oc2C)-c3ccccc3)cc1)N\C(C)=C/C(=O)c4ccc(cc4)C(F)(F)F

InChI

1S/C35H36F3N3O4/c1-4-33(43)39-22-29(40-23(2)20-32(42)26-12-14-28(15-13-26)35(36,37)38)21-25-10-16-30(17-11-25)44-19-18-31-24(3)45-34(41-31)27-8-6-5-7-9-27/h5-17,20,29,40H,4,18-19,21-22H2,1-3H3,(H,39,43)/b23-20-/t29-/m0/s1

InChI 密鑰

TYEFSRMOUXWTDN-DYQICHDWSA-N

一般說明

在肾细胞癌中，GW6471可防止细胞凋亡，并将细胞周期停滞在G0/G1。它可减少与糖酵解抑制相关的增强的脂肪酸氧化和氧化磷酸化。[1]

應用

GW6471已用于：
  • 研究过氧化物酶体增殖物激活受体（PPARs）α在全氟辛酸（PFOA）诱导的发育性心脏毒性中的作用[2]
  • 消除苯扎贝特（BZA）对肥大的保护[3]
  • 阻断乙型肝炎病毒（HBV）核心启动子的活性增强[4]

生化／生理作用

GW6471是PPARα拮抗剂，可完全抑制GW409544诱导的PPARα活化，IC50 = 0.24 μmM。GW6471可诱导可与共抑制因子有效相互作用的PPARα构象。

特點和優勢

该化合物在受体分类和信号转导手册的 核受体（PPAR） 页面上有详细描述。如需浏览其他手册页面，请点击此处。
该化合物是基因调控研究的推荐产品。点击此处，了解更多推荐基因调控产品。了解更多有关用于其他研究领域的生物活性小分子的信息，请访问sigma.com/discover-bsm。
该化合物由 GlaxoSmithKline开发。想浏览其他制药公司开发的化合物和已批准药物/候选药物目录， 请单击此处。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000389461
0000389461
0000230055
0000177499
076M4624V

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访问文档库

Hongliang Li et al.
European journal of pharmacology, 812, 155-162 (2017-07-19)
We examined the effects of the PPARα activator fenofibrate on voltage-dependent K
Shiori Ikeguchi et al.
Journal of pharmacological sciences, 138(1), 9-15 (2018-09-24)
10-oxo-trans-11-octadecenoic acid (KetoC) and 10-hydroxy-cis-12-octadecenoic acid (HYA) are long-chain fatty acids generated from linoleic acid by the gut lactic acid bacterium Lactobacillus plantarum. These fatty acids have been reported to have anti-inflammatory activity in the intestine. However, little is known
Resveratrol enhances HBV replication through activating Sirt1-PGC-1alpha-PPARalpha pathway
Shi Y, et al.
Scientific Reports, 6, 24744-24744 (2016)
Nan Xu et al.
Redox biology, 20, 87-97 (2018-10-09)
Fenofibrate, a peroxisome proliferator-activated receptors α (PPARα) agonist, reduces vascular complications of diabetic patients but its protective mechanisms are not fully understood. Here we tested the hypothesis that fenofibrate improves vascular endothelial dysfunction by balancing endothelium-dependent relaxation and contractility of
Chun Wang et al.
Environmental health perspectives, 119(12), 1739-1744 (2011-08-19)
Numerous man-made pollutants activate the aryl hydrocarbon receptor (AhR) and are risk factors for type 2 diabetes. AhR signaling also affects molecular clock genes to influence glucose metabolism. We investigated mechanisms by which AhR activation affects glucose metabolism. Glucose tolerance
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