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| 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide Basic information |
| Product Name: | 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide | | Synonyms: | 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide;GSK 3787;GSK3787/GSK-3787;Benzamide, 4-chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-;4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-benzamide GSK 3787;4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide;4-chloro-N-(2-(5-(trifluoromethyl)pyridin-2-ylsulfonyl)ethyl)benzamide;GSK3787;GSK 3787;GSK-3787 | | CAS: | 188591-46-0 | | MF: | C15H12ClF3N2O3S | | MW: | 392.78 | | EINECS: | | Product Categories: | Inhibitor;Inhibitors | | Mol File: | 188591-46-0.mol |
| 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide Chemical Properties |
| Boiling point | 585.1±50.0 °C(Predicted) | | density | 1.448±0.06 g/cm3 (20 ºC 760 Torr) | | storage temp. | 2-8°C | | solubility | DMSO: ≥10mg/mL | | form | White solid | | pka | 12.92±0.46(Predicted) | | color | white to off-white | | Stability: | Stable for 1 year for up to year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | CAS DataBase Reference | 188591-46-0 |
| Hazard Codes | Xi | | Risk Statements | 36 | | Safety Statements | 26 | | WGK Germany | 3 |
| 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide Usage And Synthesis |
| Description | GSK-3787 (188591-46-0) is a selective and irreversible antagonist of the peroxisome proliferator-activated receptor δ (PPARδ) – plC50 = 6.6. It covalently binds to Cys 249 in the PPARd binding site. | | Uses | PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers. GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5). At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells. GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.[Cayman Chemical]
| | Uses | 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. | | Biochem/physiol Actions | 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. | | References | Shearer et al., (2010)? Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist;? J. Med. Chem.?53? 1857
Palkar?et al?(2010) Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787; ?Mol.Pharmacol.?78? 419 |
| 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide Preparation Products And Raw materials |
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![4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide](/img/188591-46-0.jpg "4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide")
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