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G5797

Sigma-Aldrich

GSK0660

≥98% (HPLC)

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Synonym(s):
3-(((2-Methoxy-4-(phenylamino)phenyl)amino]sulfonyl)-2-thiophenecarboxylic acid methyl ester
Empirical Formula (Hill Notation):
C19H18N2O5S2
CAS Number:
1014691-61-2
Molecular Weight:
418.49
MDL number:
MFCD12828770
UNSPSC Code:
12352203
PubChem Substance ID:
329799945
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

originator

GlaxoSmithKline

storage temp.

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

InChI key

NDFKBGWLUHKMFY-UHFFFAOYSA-N

General description

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).

Application

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

Biochem/physiol Actions

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.

Features and Benefits

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.

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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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