A-769662

目录号 M3444 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

A-769662是一种有效的，可逆的AMPK激活剂，EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用效果。

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 660	中国库存现货
5mg	¥ 638	中国库存现货
10mg	¥ 924	中国库存现货
25mg	¥ 1848	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 98.79%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 μM.A-769662 displays selectivity towards β1 subunit-containing heterotrimers. A-769662 not only inhibits fatty acid synthesis with an IC50 of 3.2 μM but also decreases plasma glucose and triglyceride levels in vivo. The addition of A-769662 to mouse embryonic fibroblasts or primary mouse hepatocytes stimulates phosphorylation of acetyl-CoA carboxylase (ACC), effects that are completely abolished in AMPK-alpha1 (-/-)alpha2 (-/-) cells but not in TAK1 (-/-) mouse embryonic fibroblasts. Phosphorylation of AMPK and ACC in response to A-769662 is also abolished in isolated mouse skeletal muscle lacking LKB1, a major upstream kinase for AMPK in this tissue. A-769662 directly prevents the alpha (1)-isoform of the Na (+)-K (+)-ATPase which is purified from rat and human kidney cells in vitro with IC50 of 57 μM and 220 μM, respectively. Suppression of the Na (+)-K (+)-ATPase by 100 μM ouabain decreases sodium pump activity and cell surface abundance, similar to the effect of A769662 (A 769662; A-769662), without influencing the phosphorylation of AMPK and ACC.

产品使用成果展示

	数据来源	Front Physiol (2018). Figure 6. A-769662
	方法	i.p.
	细胞系/动物模型	mice
	浓度	30 mg/kg/day
	处理时间	6 weeks
	实验结果	A-769662 (30 mg/kg/day) was administered q.d. for 6 weeks. During treatment, A-769662 did not affect food intake in either chow-fed or HFD-fed mice

实验参考

体外实验*
细胞系	MEF cells
方法	Treating or not cell viability of MEF cells with A-769662 is performed as follows: harvesting cells by trypsinization and incubating with 0.5 mg/mL RNase and 50 μg/mL propidium iodine at room temperature in the dark; analyzing cell viability by flow cytometry using a FACScanto flow cytometer, using an excitation laser at 488 nm and a propidium iodine fluorescence detection at 600 nm. Cells are harvested by trypsinization, collected by centrifugation, washed in PBS and fixed overnight in 80% ethanol at -20 °C to determine the proportion of cells in each phase of the cell cycle. Subsequently, these fixed cells are centrifuged to remove the fixative and incubated for 20 minutes in the dark at room temperature in PBS containing 0.5 mg/mL RNase and 50 μg/mL propidium iodine. Flow cytometry analysis is performed as above. Using the MODFIT progra to determine the proportion of cells in G1, S, and G2 is determined . Using a camera to take Cell culture pictures at the indicated times coupled to an inverted microscope with a 20 × objective.
浓度	300 μM
处理时间	24 hours

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	Sprague Dawley rats
配制	A-769662 is dissolved in DMSO
剂量	30 mg/kg
给药处理	Administered via i.p.

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	360.39
分子式	C20H12N2O3S
CAS号	844499-71-4
溶解性（25°C）	DMSO 35 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.7748 mL	13.8739 mL	27.7477 mL
5 mM	0.555 mL	2.7748 mL	5.5495 mL
10 mM	0.2775 mL	1.3874 mL	2.7748 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Basem M Abdallah, et al. A-769662 stimulates the differentiation of bone marrow-derived mesenchymal stem cells into osteoblasts via AMP-activated protein kinase-dependent mechanism

[2] Franziska Kopietz, et al. A-769662 inhibits adipocyte glucose uptake in an AMPK-independent manner

[3] Maryam Rameshrad, et al. A-769662, a direct AMPK activator, attenuates lipopolysaccharide-induced acute heart and lung inflammation in rats

[4] Yalong Zhu, et al. A-769662 protects osteoblasts from hydrogen dioxide-induced apoptosis through activating of AMP-activated protein kinase (AMPK)

[5] Aurlie D Timmermans, et al. A-769662 potentiates the effect of other AMP-activated protein kinase activators on cardiac glucose uptake

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