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Merck
CN

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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关于此项目

经验公式(希尔记法):
C35H36F3N3O4
CAS Number:
分子量:
619.67
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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Product Name

GW6471, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

创始人

GlaxoSmithKline

储存温度

2-8°C

SMILES字符串

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 key

TYEFSRMOUXWTDN-DYQICHDWSA-N

一般描述

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。

应用

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
  • 消除苯扎贝特(BZA)对肥大的保护
  • 阻断乙型肝炎病毒(HBV)核心启动子的活性增强

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。

特点和优势

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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访问文档库

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
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
Qi Zhao et al.
Scientific reports, 7(1), 9967-9967 (2017-09-01)
Intrahepatic cholestasis induced by drug toxicity, bile salt export pump (BSEP) deficiency, or pregnancy frequently causes cholestatic liver damage, which ultimately may lead to liver fibrosis and cirrhosis. Here, the preventive and therapeutic effects of peroxisome proliferator-activated receptor α (PPARα)
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

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