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G7423

Sigma-Aldrich

GSK3787

≥98% (HPLC), white to off-white, powder

Synonyme(s) :

4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide

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About This Item

Formule empirique (notation de Hill):
C15H12ClF3N2O3S
Numéro CAS:
188591-46-0
Poids moléculaire :
392.78
Numéro MDL:
MFCD00099612
Code UNSPSC :
12352200
ID de substance PubChem :
329799963
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to off-white

Solubilité

DMSO: ≥10 mg/mL

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne SMILES 

O=S(C1=CC=C(C=N1)C(F)(F)F)(CCNC(C2=CC=C(Cl)C=C2)=O)=O

InChI

1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)

Clé InChI

JFUIMTGOQCQTPF-UHFFFAOYSA-N

Application

GSK3787 has been used to inhibit the role of peroxisome proliferator-activated receptor-delta (PPARδ), during the pre-implantation period of bovine embryonic development. It has also been used as a PPARδ-specific inhibitor in in vitro maturation (IVM) media to inhibit PPARδ.

Actions biochimiques/physiologiques

GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5). It acts by covalently modifying Cys249 within the ligand binding pocket, and has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells.
GSK3787 is known to exhibit pharmacokinetic properties.

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 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 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Stefan Kluge et al.
Biochimica et biophysica acta. Molecular and cell biology of lipids, 1866(4), 158875-158875 (2021-01-10)
The α-tocopherol-derived long-chain metabolite (α-LCM) α-13'-carboxychromanol (α-13'-COOH) is formed via enzymatic degradation of α-tocopherol (α-TOH) in the liver. In the last decade, α-13'-COOH has emerged as a new regulatory metabolite revealing more potent or even different effects compared with its
Lina Bai et al.
Acta biochimica et biophysica Sinica, 52(12), 1373-1381 (2020-11-25)
Exposure to adverse factors in utero may lead to adaptive changes in cardiac structure and metabolism, which increases the risk of chronic cardiovascular disease later in life. Studies showed that the angiotensin II type 1 receptor autoantibodies (AT1-AAs) are able
Barry G Shearer et al.
Journal of medicinal chemistry, 53(4), 1857-1861 (2010-02-05)
4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide 3 (GSK3787) was identified as a potent and selective ligand for PPARdelta with good pharmacokinetic properties. A detailed binding study using mass spectral analysis confirmed covalent binding to Cys249 within the PPARdelta binding pocket. Gene expression studies showed that
Yen-Chung Chen et al.
PloS one, 8(7), e69702-e69702 (2013-07-12)
We hypothesized that prostacyclin (PGI2) protects vascular smooth muscle cell (VSMC) against apoptosis and phenotypic switch through peroxisome proliferator-activated receptor-α (PPARα) activation and 14-3-3 upregulation. Here we showed that transfection of rat aortic VSMC, A-10, with PGI2-producing vectors, Ad-COPI, resulted
Yi Liu et al.
Cancer research, 79(5), 954-969 (2019-01-27)
APC mutations activate aberrant β-catenin signaling to drive initiation of colorectal cancer; however, colorectal cancer progression requires additional molecular mechanisms. PPAR-delta (PPARD), a downstream target of β-catenin, is upregulated in colorectal cancer. However, promotion of intestinal tumorigenesis following deletion of
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