生物活性

A-769662 belongs to the thienopyridone family. It activates the activity of purified AMPK from diffrent tissues with a dose-dependent manner. A-769662 activated the activity of AMPK extracted from human embryonic kidney cells (HEKs), rat muscle, or rat heart with EC50 values of 1.1 mM, 1.9 mM, or 2.2mM, respectively. A-769662 inhibited the synthesis of fatty acid with IC50 value of 3.2mM in primary rat hepatocytes. A769662 also has inhibition effect on the 26S proteasome with an AMPK-independent mechanism. A769662 does not inhibit the proteolytic activities of the 20S core subunit which is a novel mechanism. A769662 can cause the arrest of cell cycle by inhibiting the 26S proteasome. A-769662 activates AMPK in an allosterically manner. It also inhibits Thr-172 dephosphorylation of AMPK.

体外研究

体内研究

1% DMSO+30% polyethylene glycol+1% Tween 80

激酶实验

细胞实验

300 μM

动物实验

30 mg/kg 腹腔注射给药

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Cool B, et al, Cell Metab, 2006, 3(6), 403-416.
[2] Rajamohan, F., et al. 2010. Protein Expr. Purif. 73: 189-197.
[3] Treebak, J.T., et al. 2009. Am. J. Physiol. Cell Physiol. 297: 1041-1052.
[4] Benziane, B., et al. 2009. Am. J. Physiol. Cell Physiol. 297: 1554-1566.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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