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Merck

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
分子量:
418.49
MDL號碼:
分類程式碼代碼:
12352203
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 10 mg/mL, clear

起源

GlaxoSmithKline

儲存溫度

2-8°C

SMILES 字串

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 密鑰

NDFKBGWLUHKMFY-UHFFFAOYSA-N

一般說明

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).

應用

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.

特點和優勢

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 2

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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Bezafibrate attenuates pressure overload-induced cardiac hypertrophy and fibrosis
Xu SC, et al.
PPAR Research, 2017 (2017)
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
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
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

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