| CAS |
317318-70-0 |
| English Name |
GW 501516 |
| Synonyms |
Cardarine;Endurobol;GW 1516;GSK-516 |
| Molecular Formula |
C21H18F3NO3S2 |
| Molecular Weight |
453.5 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 1592732-453-0 |
| MDL |
MFCD09033000 |
| SMILES |
OC(COC1=CC=C(C=C1C)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)=O |
| InChIKey |
YDBLKRPLXZNVNB-UHFFFAOYSA-N |
| InChI |
InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27) |
| PubChem CID |
9803963 |
| Target Point |
PPAR |
| Passage |
Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease |
| Background |
GW 501516 is an agonist of PPARδ. |
| Biological Activity |
GW 501516是 PPARδ 的激动剂，EC50 值为 1.1 nM[1-5]。 |
| IC50 |
PPARδ:1.1nM(EC50)[1-5] |
| In Vitro |
GW 501516在小鼠培养的近端小管(mProx)细胞中发挥抗炎作用。 GW 501516以剂量依赖性方式抑制棕榈酸和TNFα诱导的MCP-1 mRNA表达增加[3]。 |
| In Vivo |
GW 501516导致骨形成受损，导致OVX大鼠的骨密度降低和骨特性恶化[2]。 GW 501516在蛋白质超负荷小鼠肾病模型中减轻间质炎症和近端肾小管细胞损伤[3]。 GW 501516治疗增强了训练和未训练小鼠的跑步耐力和琥珀酸脱氢酶(SDH)阳性肌纤维的比例[4]。 |
| Cell Experiment |
将GW 501516溶解在DMSO中。通过在0.2％FCS DMEM中孵育9小时使细胞饥饿，然后与GW 501516一起预孵育，终浓度为2.5和5μM，或0.05％DMSO作为对照3小时，然后用150μM棕榈酸酯刺激进行刺激12小时达到8.0％BSA [3]。 |
| Animal Experiment |
大鼠：将12周龄的雌性Sprague Dawley大鼠分配到假手术组和3个OVX组;高剂量GW 501516(OVX-GW5)，低剂量GW 501516(OVX-GW1)和对照组(OVX-CTR)。动物每天通过管饲法接受GW 501516或载体(甲基纤维素)4个月。通过股骨，脊柱和全身的双X射线吸收测定法评估骨矿物质密度(BMD)[2]。小鼠：将小鼠随机分配到不同的组并接受治疗性饮食和治疗。通过将GW 501516均匀添加至对照饮食至终浓度为0.04％w/w来制备含有GW 501516的啮齿动物饮食。在对照饮食中，总卡路里的10％来自脂肪(来自大豆油的5.5％和来自猪油的4.5％)[3]。 |
| Data Literature Source |
[1]. Wei ZL，et al. 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]. Mosti MP，et al. Effects of the peroxisome proliferator-activated receptor (PPAR)-δ agonist GW 501516 on bone and muscle in ovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89.
[3]. Yang X，et al. GW 501516，a PPARδ agonist，ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition of TAK1-NFκB pathway in mice. PLoS One. 2011;6(9):e25271.
[4]. Chen W，et al. A metabolomic study of the PPARδ agonist GW 501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884.
[5]. Ji Y，et al. PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. Front Pharmacol. 2018 Jun 28;9:648. |
| Unit |
Piece |
| Specification |
5mg 10mg |
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