FK614 is an orally active, potent, selective PPARγ modulator (SPPARM). FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 is a nonthiazolidinedione insulin sensitizer. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes[1][2][3].
FK614 (0.1~10000 nM; 24 hours; CV-1 cells) activates PPARγ-dependent transcription in a concentration-dependent manner. FK614 (0~0.1 μM; 5 days; 3T3-L1 adipocytes) makes triglyceride content increased in a concentration-dependent manner. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 is an insulin sensitizer potentially for treatment of postherpetic neuralgia[1][2].
FK614 (0.32~3.2 mg/kg; p.o.; 14 days) dose-dependently reduces plasma glucose level[3].FK614 (0.1~10 mg/kg; p.o.; 14 days) improves the impaired glucose tolerance[3].
[1]. Fujimura T, et al. A selective peroxisome proliferator-activated receptor gamma modulator with distinct fat cell regulation properties. J Pharmacol Exp Ther. 2006;318(2):863-871.
[2]. Fujimura T, et al. FK614, a novel peroxisome proliferator-activated receptor gamma modulator, induces differential transactivation through a unique ligand-specific interaction with transcriptional coactivators. J Pharmacol Sci. 2005;99(4):342-352.