GW501516

GW501516化学性质

熔点 :134-136°C
沸点 :584.5±60.0 °C(Predicted)
密度 :1.42±0.1 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :DMSO: soluble20mg/mL, clear
形态 :powder
酸度系数(pKa) :3.17±0.10(Predicted)
颜色 :white to beige
BRN :18515150
稳定性 :Light Sensitive
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)
InChIKey :YDBLKRPLXZNVNB-UHFFFAOYSA-N
SMILES :C(O)(=O)COC1=CC=C(SCC2SC(C3=CC=C(C(F)(F)F)C=C3)=NC=2C)C=C1C
CAS 数据库 :317318-70-0

安全信息

GW501516性质、用途与生产工艺

生物活性 GW 501516 (GW 1516) 是 PPARδ 的激动剂，EC50 值为 1.1 nM。
靶点
Target Value
PPARδ
(Cell-free assay) 1 nM(Ki)
体外研究

GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC ₅₀ of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.
体内研究

GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

GW501516上下游产品信息

上游原料

下游产品

GW501516 试剂级价格

GW501516生产厂家

317318-70-0, GW501516相关搜索:

Target	Value
PPARδ (Cell-free assay)	1 nM(Ki)