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Submit ReviewGW 7647
说明： Highly selective, potent PPARα agonist. Orally active
化学名： 2-[[4-[2-[[(Cyclohexylamino)carbonyl](4-cyclohexylbutyl)amino]ethyl]phenyl]thio]-2-methylpropanoic acid
纯度： ≥99% (HPLC)
生物活性 for GW 7647
GW 7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro. Has lipid-lowering effects following oral administration in vivo. Reduces NO production in macrophages; exhibits anti-inflammatory properties.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 for GW 7647
GW 7647 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GW 7647
| 分子量 | 502.75 |
| 公式 | C29H46N2O3S |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 265129-71-3 |
| PubChem ID | 3392731 |
| InChI Key | PKNYXWMTHFMHKD-UHFFFAOYSA-N |
| Smiles | CC(C)(SC1=CC=C(CCN(CCCCC2CCCCC2)C(=O)NC2CCCCC2)C=C1)C(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GW 7647
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 12.57 | 25 | |
| DMSO | 50.27 | 100 |
制备储备液 for GW 7647
以下数据基于产品分子量 502.75。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.99 mL | 9.95 mL | 19.89 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.98 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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产品说明书 for GW 7647
参考文献 for GW 7647
参考文献是支持产品生物活性的出版物。
Brown et al (2001) Identification of a subtype selective human PPARα agonist through parallel-array synthesis. Bioorg.Med.Chem.Lett. 11 1225 PMID: 11354382
Cunard et al (2002) Regulation of cytokine expression by ligands of peroxisome proliferator activated receptors. J.Immunol. 168 2795 PMID: 11884448
Muoio et al (2002) Peroxisome proliferator-activated receptor-α regulates fatty acid utilization in primary human skeletal muscle cells. Diabetes 51 901 PMID: 11916905
Paukkeri et al (2007) PPARalpha agonists inhibit nitric oxide production by enhancing iNOS degradation in LPS-treated macrophages. Br.J.Pharmacol. 152 1081 PMID: 17891158
If you know of a relevant reference for GW 7647, please let us know.
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关键词: GW 7647, GW 7647 supplier, selective, potent, PPARα, PPARalpha, agonists, Orally, active, Peroxisome, Proliferator-activating, Receptors, PPAR, GW7647, GlaxoSmithKline, GSK, anti-inflammatory, 1677, Tocris Bioscience
8 篇 GW 7647 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GW 7647 的部分引用包括：
Fellous et al (2020) Phytocannabinoids promote viability and functional adipogenesis of bone marrow-derived mesenchymal stem cells through different molecular targets Biochemical Pharmacology 175 PMID: 32061773
Ropero et al (2009) Rapid non-genomic regulation of Ca2+ signals and Ins secretion by PPAR alpha ligands in mouse pancreatic islets of Langerhans. J Endocrinol 200 127 PMID: 19017711
Mattsson et al (2015) Metabolic Profiling of Chicken Embryos Exposed to Perfluorooctanoic Acid (PFOA) and Agonists to Peroxisome Proliferator-Activated Receptors. PLoS One 10 e0143780 PMID: 26624992
Hatano et al (2010) Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators. Cell Commun Signal 125 160 PMID: 19818482
Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. Bioorg Med Chem 287 25038 PMID: 22685301
Guo et al (2018) Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis. Nat Med 24 360 PMID: 29377004
Moreno-Santos et al (2014) Computational and biological evaluation of N-octadecyl-N'-propylsulfamide, a selective PPARα agonist structurally related to N-acylethanolamines. PLoS One 9 e92195 PMID: 24651609
Yu et al (2013) Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. J Allergy Clin Immunol 21 4266 PMID: 23688559
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GW 7647 的评论
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PPAR alpha agonists inhibit nitric oxide production by enhancing iNOS degradation in LPS-treated macrophages..
By
GAJANAN KATKAR on 12/07/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： J774 murine macrophages
GW7647 is the most potent PPARalpha agonist that reduces LPS-induced iNOS expression and NO production in macrophages by enhancing iNOS protein degradation through the proteasome pathway. Concentration 3, 10 and 30 uM showed dose-dependent inhibition.