GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
IC50 Value: 1 nM(EC50)
Target: PPARβ/δ
in vitro: GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, GW501516 is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. GW 501516 reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity.
in vivo: GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. GW501516 induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice.

A-966492
AG14361
Aleglitazar
AZD-2461
Balaglitazone
BMN-673
BSI-201
FH535
G007-lk
GSK3787
GW1929
GW9662
INO-1001
JW 55
L-185041
MK4827
PJ34
T0070907
UPF 1069
XAV-939