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G5797

Sigma-Aldrich

GSK0660

≥98% (HPLC)

别名:

3-(((2-Methoxy-4-(phenylamino)phenyl)amino]sulfonyl)-2-thiophenecarboxylic acid methyl ester

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About This Item

经验公式（希尔记法）:
C19H18N2O5S2
CAS号:
1014691-61-2
分子量:
418.49
MDL编号:
MFCD12828770
UNSPSC代码:
12352203
PubChem化学物质编号:
329799945
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

创始人

GlaxoSmithKline

储存温度

2-8°C

SMILES字符串

COC(=O)c1sccc1S(=O)(=O)Nc2ccc(Nc3ccccc3)cc2OC

InChI

1S/C19H18N2O5S2/c1-25-16-12-14(20-13-6-4-3-5-7-13)8-9-15(16)21-28(23,24)17-10-11-27-18(17)19(22)26-2/h3-12,20-21H,1-2H3

InChI key

NDFKBGWLUHKMFY-UHFFFAOYSA-N

一般描述

GSK0660 has antiangiogenic property in oxygen-induced retinopathy. It also regulates tumor necrosis factor-α (TNFα)-induced inflammation in human retinal microvascular endothelial cells (HRMECs).

应用

GSK0660 has been used to study the effects of bezafibrate (BZA) on hypertrophy.

生化/生理作用

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (160 nM). GSK0660 is nearly inactive on PPARα and PPARγ with IC50s greater than 10 μM.
GSK0660 is a potent PPARβ/δ antagonist with pIC50 of 6.8 (160 nM).

特点和优势

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Nuclear Receptors (PPARs) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000031359
0000023120
BGBC2273V
041M4610V
108K46073

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Shumei Ding et al.
Experimental cell research, 382(1), 111455-111455 (2019-06-05)
Diabetic nephropathy (DN) is one of the most severe complications of diabetes mellitus. The pathomolecular events behind DN remain uncertain. Peroxisome proliferator-activated receptors (PPARs) play essential functions in the development of DN. Meanwhile, 20-hydroxyeicosatetraenoic acid (20-HETE) also plays central roles
Bezafibrate attenuates pressure overload-induced cardiac hypertrophy and fibrosis
Xu SC, et al.
PPAR Research, 2017 (2017)
Eun Jeong Jeon et al.
Scientific reports, 9(1), 1236-1236 (2019-02-06)
Telmisartan is a well-known anti-hypertensive drug acting as an angiotensin 2 receptor blocker (ARB), but it also possesses partial PPARγ agonistic activity and induces insulin sensitivity. In the present study, we investigated the effects of telmisartan on macrophage polarization in
RNA-seq identifies a role for the PPARbetadelta inverse agonist GSK0660 in the regulation of TNFalpha-induced cytokine signaling in retinal endothelial cells
Savage SR, et al.
Molecular Vision, 21, 568-568 (2015)
Ali Khorasani et al.
The International journal of neuroscience, 129(11), 1053-1065 (2019-06-20)
Aim: Alzheimer's disease (AD) is characterized by oxidative stress, neuroinflammation and progressive cognitive decline. Abscisic acid (ABA) is produced in a variety of mammalian tissues, including brain. It has anti-inflammatory and antioxidant effects and elicits a positive effect on spatial
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