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编 号:F747560
分子式:C23H23ClN2O5
分子量:442.89
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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生物活性:
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.

体内研究:
PF-739 (30-1000 mg/kg;口服或皮下注射;单剂量) 有效激活 C57BL/6 小鼠肝细胞和骨骼肌中的 AMPK,降低血浆葡萄糖水平。Animal Model:C57BL/6 mice.
Dosage:30, 100, 300 or 1000 mg/kg.
Administration:Oral gavage or subcutaneous injection; single does.
Result:Increased AMPK activity in skeletal muscle, AMPK phosphorylation in liver tissue and the expression of transcription factors Ppargc1a, Nr4a1, Nr4a3 in glucose metabolism pathway, and decreased plasma insulin and blood glucose.

体外研究:
PF-739 激活 α2β1γ1、α2β2γ1、α1β1γ1 和 α1β2γ1,EC50 值分别为 5.23 nM、42.2 nM、8.99 nM 和 126 nM。PF-739 (0-1000 nM) 以剂量依赖性方式增加原代大鼠肝细胞和原代人心肌细胞系的肌管中 AMPK 底物磷酸化。
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