GW-501516 PPAR delta agonist PPARδ受体激动剂 317318-70-0

保存条件 ：零下20度

保质期 ：3年

英文名 ：GW-501516

库存 ：大量

供应商 ：上海惠诚生物科技有限公司

CAS号 ：317318-70-0

规格 ：5 mg/25 mg

GW-501516 (317318-70-0) is a potent and selective PPARδ (NR1C2) agonist, EC₅₀=1.2 nM and 1000-fold selective over other PPAR subtypes.¹  Induces apolipoprotein A1-mediated cholesterol efflux in vitro.¹ Improves hematopoietic stem cell maintenance.² Prevents downregulation of AMPK caused by a high-fat diet in liver and increases fatty acid oxidation.³ Upregulates human Sirt1 via Sp1 activation.⁴ Along with exercise, GW-501516 synergistically increases running endurance.⁵
gf -501516(317318-70-0)是一种强效且选择性的PPARδ (NR1C2)激动剂，EC50=1.2 nM，比其他PPAR亚型具有1000倍的选择性 体外诱导载脂蛋白a1介导的胆固醇外排 改善造血干细胞的维持 防止肝脏高脂饮食引起的AMPK下调，增加脂肪酸氧化 4 .通过Sp1激活上调人类Sirt1 随着运动，GW-501516协同提高跑步耐力。 

References/Citations:

1) Oliver et al. (2001), A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport; Proc. Natl. Acad. Sci. USA, 98 5306
2) Ito et al. (2012), A PML-PPAR-δ pathway for fatty acid oxidation regulates hematopoietic stem cell maintenance; Nat. Med., 18 1350
3) Barroso et al. (2011), The PPARβ/δ activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1α-Lipin 1-PPARα pathway leading to increased fatty acid oxidation. Endocrinology, 152 1848
4) Okazaki et al. (2010), PPAR beta/delta regulates the human SIRT1 gene transcription via Sp1; Endocr. J., 57 403
5) Narkar et al. (2008), AMPK and PPARdelta agonists are exercise mimetics; Cell, 134 405

CAS:
317318-70-0
Catalog Number:
10-1542
Activity:
PPAR delta agonist
Chemical Name:
2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazoyl]methyl]thio]phenoxy]acetic acid
Molecular Weight:
453.50
Molecular Formula:
C₂₁H₁₈F₃NO₃S₂
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT