HWL-088

2378617-96-8

366.38

DMSO : 250 mg/mL (ultrasonic)

Cell Cycle/DNA Damage, GPCR/G Protein

HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC₅₀ of 18.9 nM) with moderate PPARdelta activity (EC₅₀ of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects^[1][2]. IC50 & Target: EC50: 18.9 nM (FFA1/GPR40); 570.9 nM (PPARdelta)^[2] In Vitro: HWL-088 (0.3 uM and 3uM) significantly increases insulin secretion fromMIN6 cells at 25 mM but not at 2 mM glucose. HWL-088 reveales a dose-dependent insulinotropic effect in the presence of 25-mM glucose^[2]. In Vivo: HWL-088 (40 mg/kg; oral gavage; daily; for 30 days; ob/ob mice) treatment improves beta-cell function by up-regulation of pancreas duodenum homeobox-1, reduces fat accumulation in adipose tissue and alleviated fatty liver in ob/ob mice. The effect of HWL-088 involves a reduction in hepatic lipogenesis and oxidative stress, increased lipoprotein lipolysis, glucose uptake, mitochondrial function and fatty acid beta-oxidation^[2].