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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
FK614 是一种非噻唑烷二酮 (TZD) 型选择性 PPARγ 调节剂 (SPPARM)。FK614 是一种 PPARγ 激动剂,显示出强大的抗糖尿病活性。FK614 在脂肪细胞分化的各个阶段对 PPARγ 的激活有不同的影响。FK614 可用于研究高血糖、高甘油三酯血症、糖耐量异常和 2 型糖尿病。
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
In Vitro
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. FK614 is a non-TZD insulin sensitizer. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
FK614 (0.32~3.2 mg/kg; p.o.; 14 days) dose-dependently reduces plasma glucose level. FK614 (0.1~10 mg/kg; p.o.; 14 days) improves the impaired glucose tolerance. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: db/db Mice Dosage: 0.1~10 mg/kg Administration: P.o. Result: Improved the impaired glucose tolerance. Animal Model: db/db Mice Dosage: 0.32~3.2 mg/kg Administration: P.o. Result: Dose-dependently reduced plasma glucose level.
IC50& Target:PPAR-γ
| ALogP | 5.3 |
|---|