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Submit ReviewGW 501516 is a potent and selective PPARδ agonist (EC50 = 1.2 nM). Displays <1000-fold selectivity over other PPAR subtypes. Increases ABC A1 transporter expression and induces apolipoprotein A1-mediated cholesterol efflux in vitro. Also increase serum HDL cholesterol and lowers small, dense LDL levels in obesity in vivo models.
分子量 | 453.5 |
公式 | C21H18F3NO3S2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 317318-70-0 |
PubChem ID | 9803963 |
InChI Key | YDBLKRPLXZNVNB-UHFFFAOYSA-N |
Smiles | CC1=CC(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)=CC=C1OCC(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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 45.35 | 100 | |
ethanol | 22.68 | 50 |
以下数据基于产品分子量 453.5。 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 | 2.21 mL | 11.03 mL | 22.05 mL |
5 mM | 0.44 mL | 2.21 mL | 4.41 mL |
10 mM | 0.22 mL | 1.1 mL | 2.21 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
参考文献是支持产品生物活性的出版物。
Oliver et al (2001) A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc.Natl.Acad.Sci.USA. 98 5306 PMID: 11309497
Ito et al (2016) Self-renewal of a purified Tie2+ hematopoietic stem cell population relies on mitochondrial clearance. Science 354 1156 PMID: 27738012
If you know of a relevant reference for GW 501516, please let us know.
关键词: GW 501516, GW 501516 supplier, GW501516, Potent, selective, PPARδ, agonists, agonism, reverse, cholesterol, transporter, ATP-binding, cassette, A1, obesity, peroxisome, proliferator-activated, receptors, delta, PPARdelta, Receptors, 5674, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GW 501516 的部分引用包括:
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
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