SML4244
GSK0660
≥98% (HPLC)
别名:
3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester, Methyl 3-({[2-(methoxy)-4 phenyl]amino}sulfonyl)-2-thiophenecarboxylate, GSK 0660, GSK-0660
生化/生理作用
Potent and selective PPARdelta (PPARbeta) antagonist.
GSK0660 is a potent and selective PPARdelta (PPARbeta) agonist (IC50 = 300 nM against GW1516-induced PPARβ/δ reporter activity; IC50 = 155 nM vs >10 µM for PPARα and PPARγ by GW1516 displacement binding assays). GSK0660 effectively antagonizes PPARβ/δ agonist GW501516 (GW1516)-induced target genes expression in multiple cell types, including HuH7, rat L6 myotubes, and mouse BMDMs (1-10 nM GW1516, 100-1000 nM GSK0660).
GSK0660 is a potent and selective PPARdelta (PPARbeta) agonist (IC50 = 300 nM against GW1516-induced PPARβ/δ reporter activity; IC50 = 155 nM vs >10 µM for PPARα and PPARγ by GW1516 displacement binding assays). GSK0660 effectively antagonizes PPARβ/δ agonist GW501516 (GW1516)-induced target genes expression in multiple cell types, including HuH7, rat L6 myotubes, and mouse BMDMs (1-10 nM GW1516, 100-1000 nM GSK0660).
法规信息
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历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Bibimaryam Khan et al.
European journal of pharmacology, 972, 176565-176565 (2024-04-11)
Blockade of PD-1/PD-L1 immune checkpoint is wildly used for multiple types of cancer treatment, while the low response rate for patients is still completely unknown. As nuclear hormone receptor, PPARδ (peroxisome-proliferator-activated receptor) regulates cell proliferation, inflammation, and tumor progression, while
Barry G Shearer et al.
Molecular endocrinology (Baltimore, Md.), 22(2), 523-529 (2007-11-03)
The identification of small molecule ligands for the peroxisome proliferator-activated receptors (PPARs) has been instrumental in elucidating their biological roles. In particular, agonists have been the focus of much of the research in the field with relatively few antagonists being
Andrea Antonosante et al.
Biological research, 56(1), 27-27 (2023-05-25)
The underlying mechanism of Parkinson's disease are still unidentified, but excitotoxicity, oxidative stress, and neuroinflammation are considered key actors. Proliferator activated receptors (PPARs) are transcription factors involved in the control of numerous pathways. Specifically, PPARβ/δ is recognized as an oxidative
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