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抑制剂/激活剂

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凋亡与自噬

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A-769662

A-769662是一种有效的，可逆的AMPK激活剂，在无细胞试验中EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用。

货号：
TK0288
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	844499-71-4
生物活性	A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
分子式	C20H12N2O3S
分子量	360.39
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 50 mg/mL (138.74 mM; ultrasonic and warming and heat to 80°C)
体内研究	A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange ratio (RER) in the SD rat. There are 33% and 58% reductions of malonyl CoA levels in livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g), respectively. A-769662 (30 mg/kg, b.i.d.) significantly decreases fed plasma glucose (30%-40% reduction), while the lower doses (3 and 10 mg/kg) of A-769662 had no effect on the in diabetic ob/ob mice.
体外研究	A-769662 is equally potent in activating the baculovirus expressed α1,β1,γ1 recombinant isoform of AMPK (EC50=0.7 μM). A-769662 and A-592107 activate AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 μM, 1.9 μM, or 1.1 μM, respectively. A-769662 activates endogenous AMPK in LKB1-expressing (HEK293) and LKB1-deficient (CCL13) cells. A-769662 allosterically activates AMPK complexes containing γ1 harboring a substitution of arginine residue 298 to glycine (R298G). A-769662 inhibits dephosphorylation of Thr-172 in the mutant γ1-containing complexes to a similar degree as seen in the wild-type complexes. A769662 (300 μM) has toxic effects on MEF cells. A769662 reversibly inhibits the proteasomal activity.
文献	暂无相关参考文献
纯度及产品资料	98%

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