For research use only. Not for therapeutic Use.
FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes[1][2].
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[1].
FK614 is an insulin sensitizer potentially for treatment of postherpetic neuralgia. FK614 is a non-TZD insulin sensitizer[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].
| Catalog Number | I006363 |
| CAS Number | 193012-35-0 |
| Synonyms | 3-[(2,4-dichlorophenyl)methyl]-2-methyl-N-pentylsulfonylbenzimidazole-5-carboxamide |
| Molecular Formula | C21H23Cl2N3O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H23Cl2N3O3S/c1-3-4-5-10-30(28,29)25-21(27)15-7-9-19-20(11-15)26(14(2)24-19)13-16-6-8-17(22)12-18(16)23/h6-9,11-12H,3-5,10,13H2,1-2H3,(H,25,27) |
| InChIKey | UYGZODVVDUIDDQ-UHFFFAOYSA-N |
| SMILES | CCCCCS(=O)(=O)NC(=O)C1=CC2=C(C=C1)N=C(N2CC3=C(C=C(C=C3)Cl)Cl)C |
| Reference | [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. [3]. Minoura H, et al. Ameliorating effect of FK614, a novel nonthiazolidinedione peroxisome proliferator-activated receptor gamma agonist, on insulin resistance in Zucker fatty rat. Eur J Pharmacol. 2005;519(1-2):182-190. |
