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G5797

Sigma-Aldrich

GSK0660

≥98% (HPLC)

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C19H18N2O5S2
CAS-Nummer:
1014691-61-2
Molekulargewicht:
418.49
MDL-Nummer:
MFCD12828770
UNSPSC-Code:
12352203
PubChem Substanz-ID:
329799945
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 10 mg/mL, clear

Ersteller

GlaxoSmithKline

Lagertemp.

2-8°C

SMILES String

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

InChIKey

NDFKBGWLUHKMFY-UHFFFAOYSA-N

Allgemeine Beschreibung

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).[1]

Anwendung

GSK0660 has been used to study the effects of bezafibrate (BZA) on hypertrophy.[2]

Biochem./physiol. Wirkung

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).

Leistungsmerkmale und Vorteile

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 2

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)

Hier finden Sie alle aktuellen Versionen:

Analysenzertifikate (COA)

Lot/Batch Number
BGBC2273V
041M4610V
108K46073
108K46072
108K46071

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Sigma-Aldrich

C7081

WY-14643

T0070907 ≥98% (HPLC)

Sigma-Aldrich

T8703

T0070907

Rosiglitazon ≥98% (HPLC)

Sigma-Aldrich

R2408

Rosiglitazon

Albumin aus Rinderserum fatty acid free, low endotoxin, lyophilized powder, BioReagent, suitable for cell culture, ≥96% (agarose gel electrophoresis)

Sigma-Aldrich

A8806

Albumin aus Rinderserum

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
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
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)
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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Nuclear Receptors: PPARs

Peroxisome proliferator activated receptors (PPARs) are ligand-activated transcription factors related to hormone receptors, influencing gene expression.

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