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G5797

Sigma-Aldrich

GSK0660

≥98% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill) :
C19H18N2O5S2
Numéro CAS:
1014691-61-2
Poids moléculaire :
418.49
Numéro MDL:
MFCD12828770
Code UNSPSC :
12352203
ID de substance PubChem :
329799945
Nomenclature NACRES :
NA.77

Essai

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 10 mg/mL, clear

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne SMILES 

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

Clé InChI

NDFKBGWLUHKMFY-UHFFFAOYSA-N

Description générale

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]

Application

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

Actions biochimiques/physiologiques

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).

Caractéristiques et avantages

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)

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Certificats d'analyse (COA)

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

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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
Gwendoline Degueurce et al.
EMBO molecular medicine, 8(8), 919-936 (2016-06-03)
Although excessive exposure to UV is widely recognized as a major factor leading to skin perturbations and cancer, the complex mechanisms underlying inflammatory skin disorders resulting from UV exposure remain incompletely characterized. The nuclear hormone receptor PPARβ/δ is known to
Bijoy Chellan et al.
Scientific reports, 8(1), 11954-11954 (2018-08-12)
Enzyme modified non-oxidative LDL (ELDL) is effectively taken up by vascular smooth muscle cells (SMC) and mediates transition into foam cells and produces phenotypic changes in SMC function. Our data show that incubation of human coronary artery SMC (HCASMC) with
Daniel Morales-Cano et al.
Clinical science (London, England : 1979), 130(20), 1823-1836 (2016-07-15)
PPARβ/δ activation protects against endothelial dysfunction in diabetic models. Elevated glucose is known to impair cAMP-induced relaxation and Kv channel function in coronary arteries (CA). Herein, we aimed to analyse the possible protective effects of the PPARβ/δ agonist GW0742 on
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