推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
−20°C
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)
InChI key
YDBLKRPLXZNVNB-UHFFFAOYSA-N
应用
GW501516作为过氧化物酶体增殖物激活受体(PPAR)δ激动剂的应用：
- 用于处理L6分化肌管细胞，检测其在温和缺氧条件下对游离脂肪酸(FFA)摄取的影响
- 在类器官培养基中检测其对PR结构域蛋白16(Prdm16)缺失的肠干细胞自我更新的影响
- 作为脱脂培养基组分，用于原代人肝细胞(PHH)培养
利用小鼠模型，GW501516对于突变驱动的结直肠癌肿瘤生成和肿瘤侵袭的作用已得到研究。
生化/生理作用
GW501516是一种选择性过氧化物酶体增殖物激活受体δ（PPARδ）激动剂，对于PPARδ具有高亲和性（Ki = 1 nM）和高功效（EC50 = 1 nM），并相对于PPARα和PPARγ1具有> 1000倍的选择性。GW501516可激活一些同样可通过运动激活的通路，并作为肥胖、糖尿病、血脂异常和心血管疾病的一种潜在治疗方法而被研究。然而，GW501516也在大鼠癌症中有所提高。
由GW501516所激活的PPARδ可通过脂肪组织和骨骼肌中脂肪酸的代谢而延缓体重的增加。GW501516可导致高密度脂蛋白胆固醇和载脂蛋白A（apoA）水平的升高，以及低密度脂蛋白胆固醇、apoB和甘油三酯水平的降低。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
监管及禁止进口产品
Activation of peroxisome proliferator-activated receptor-δ by GW501516 prevents fatty acid-induced nuclear factor-κB activation and insulin resistance in skeletal muscle cells.
Coll T, et al.
Endocrinology, 151(4), 1560-1569 (2010)
Pleotropic effects of PPARD accelerate colorectal tumor progression and invasion.
Liu Y, et al.
bioRxiv, 325001-325001 (2018)
Lipid effects of peroxisome proliferator-activated receptor-δ agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.
Olson E J, et al.
Arteriosclerosis, Thrombosis, and Vascular Biology, 32(9), 2289-2294 (2012)
Yi Ling Low et al.
Molecular pharmaceutics, 17(3), 873-884 (2020-01-17)
Brain levels of docosahexaenoic acid (DHA), an essential cognitively beneficial fatty acid, are reduced in Alzheimer's disease (AD). We have demonstrated in an AD mouse model that this is associated with reduced blood-brain barrier (BBB) transport of DHA and lower
Buqing Ye et al.
The EMBO journal, 39(13), e103786-e103786 (2020-05-26)
Lgr5+ intestinal stem cells (ISCs) exhibit self-renewal and differentiation features under homeostatic conditions, but the mechanisms controlling Lgr5 + ISC self-renewal remain elusive. Here, we show that the chromatin remodeler SRCAP is highly expressed in mouse intestinal epithelium and ISCs. Srcap deletion
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