| CAS NO: | 317318-70-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 453.5 |
| Cas No. | 317318-70-0 |
| Formula | C21H18F3NO3S2 |
| Solubility | insoluble in H2O; ≥18.05 mg/mL in DMSO; ≥44.6 mg/mL in EtOH |
| Chemical Name | 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid |
| Canonical SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
GW501516是过氧化物酶体增殖物激活受体δ（PPARδ）的亚型选择性小分子激动剂，Ki值为1.1 nM[1]。
GW501516是通过组合化学和基于结构的药物设计发现的，可以作为一种理想的化学工具研究广泛表达的PPAR功能。在基于细胞的转染实验中，GW501516诱导GAL4响应性报告基因的表达，EC50值为1.2 nM。相较于其他亚型，GW501516对PPARδ具有高达1000倍的选择性。PPARδ在许多组织表达，有助于胆固醇流动，并且与类视黄醇X受体(RXR)相互作用。作为PPARδ激动剂，GW501516可以增加ABCA1的表达以及载脂蛋白A 1（apoA1）特异性胆固醇流出。在患有人代谢疾病的灵长类动物模型中，GW501516提升HDLc水平，降低空腹甘油三脂含量。GW501516也产生较少的，但较大的LDL和VLDL颗粒，导致动脉粥样硬化较少的脂质成分。此外，GW501516部分纠正了灵长类动物的高胰岛素血症，对血糖控制没有产生副作用[1,2]。
参考文献：
[1] Wei ZL, Kozikowski AP. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8.
[2] Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5306-11.
| Cell experiment:[1] | |
Cell lines | THP1 macrophages, 1BR3N human skin fibroblasts and FHS74 human intestinal cells |
Reaction Conditions | 100 nM GW501516 |
Applications | In macrophages, fibroblasts, and intestinal cells, GW501516 increased expression of the reverse cholesterol transporter ATP-binding cassette A1 (ABCA1) and induced apolipoprotein A1-specific cholesterol efflux. These results suggest that GW501516 may promote cholesterol efflux from multiple tissues by increasing expression of the reverse cholesterol transporter ABCA1. |
| Animal experiment:[2] | |
Animal models | A rat model of non-alcoholic fatty liver disease induced by a high-fat diet |
Dosage form | 10 mg/kg Once daily by oral route for 4 weeks |
Applications | After 4 weeks of treatment with GW501516, the hepatosomatic index was almost reduced to the level of the normal control group. In addition, a significant decrease in body mass index was observed in the rats that were treated with GW501516 for 4 weeks. GW501516 was found to alleviate non-alcoholic fatty liver disease by modulating glucose and fatty acid metabolic enzymes in a rat model. |
Note | The technical data provided above is for reference only. |
References: 1. Oliver WR Jr, Shenk JL, Snaith MR, et al. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proceedings of the National Academy of Sciences of the United States of America, 2001, 98(9): 5306-5311. 2. Li X, Li J, Lu X, et al. Treatment with PPARδ agonist alleviates non-alcoholic fatty liver disease by modulating glucose and fatty acid metabolic enzymes in a rat model. International Journal of Molecular Medicine, 2015, 36(3): 767-775. | |
| Description | GW501516是PPARβ的强效选择性激动剂，EC50值为1.1 nM。 | |||||
| 靶点 | PPARβ | |||||
| IC50 | 1.1 nM (EC50) | |||||
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