PF-739

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型强效泛 AMPK 激活剂，对所有 AMPK 异三聚体具有相似的效力。

A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 121 nM, potently inhibits de novo lipogenesis (IC50=25 nM) in primary rat hepatocytes; increases PGC1a transcription and mitochondrial content, effectively activats AMPK in hepatocytes and in skeletal muscle; caused a rapid lowering of plasma glucose levels with no impact on hepatic glucose production in diabetic mice.

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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.

PF 739 | PF739

Membrane Transporter/Ion Channel

AMPK

AMPK

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1852452-14-2

442.896

C23H23ClN2O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (225.79 mM)

O[C@H]1[C@](OC[C@H]2OC3=NC4=CC(C5=CC=C(C6(CO)CC6)C=C5)=C(Cl)C=C4N3)([H])[C@]2([H])OC1

(3R,3aR,6R,6aR)-6-((6-chloro-5-(4-(1-(hydroxymethyl)cyclopropyl)phenyl)-1Hbenzo[d]imidazol-2-yl)oxy)hexahydrofuro[3,2-b]furan-3-ol

(-20℃)

With Ice Pack

≥ 2 years