1. Epigenetics PI3K/Akt/mTOR Metabolic Enzyme/Protease
  2. AMPK Acetyl-CoA Carboxylase
  3. AMPK activator 18

AMPK activator 18 是一种强效的靶向含 β2 亚型的 AMPK 复合物的变构激活剂。AMPK activator 18 可激活含 α2 的 AMPK α2β2γ1α2β2γ3 复合物,其 EC50 值分别为 17.2 和 82.1 nM。AMPK activator 18 可激活细胞中的 β2-AMPK,并促进离体骨骼肌的葡萄糖摄取。AMPK activator 18 可诱导乙酰辅酶 A 羧化酶 (ACC) 和 AMPK α-T172 的磷酸化。AMPK activator 18 可用于 2 型糖尿病的相关研究。

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AMPK activator 18

AMPK activator 18 Chemical Structure

CAS No. : 1364692-88-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes[1].

IC50 & Target[1]

AMPK α2β2γ1

17.2 nM (EC50)

α2β2γ3

82.1 nM (EC50)

体外研究
(In Vitro)

AMPK activator 18 可强效且选择性地激活含 α2 的 AMPK 复合物,尤其是在骨骼肌中高表达的 α2β2γ1 和 α2β2γ3 复合物,其 EC50 值分别为 17.2 ± 1.6 nM 和 82.1 ± 1.3 nM,且其激活作用依赖于 β2-D111 残基,而非 β2 的 N 端螺旋[1]
AMPK activator 18 (0.03-10 μM; 1 h) 可通过不依赖细胞内 AMP/ATP 比值变化或 AMPK α-T172 磷酸化的变构机制,在分化的 C2C12 肌管和重构 β2 的 iMEF 中激活 AMPK 信号通路,并诱导呈剂量依赖性的 ACC 磷酸化[1]
AMPK activator 18 (1-2 μM) 可提高肘肌中 ACC 磷酸化水平及 AMPK α-T172 磷酸化水平[1]
AMPK activator 18 (10 μM) 可降低比目鱼肌和趾长伸肌对 2-脱氧葡萄糖 (2DG) 的摄取[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: β2-expressing b1/2 dKO iMEFs
Concentration: 1 μM; 10 μM
Incubation Time: 1 h
Result: Induced a significant increase in ACC phosphorylation without altering AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 1 μM.
Induced ACC phosphorylation associated with an increase in AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 10 μM.
分子量

471.90

Formula

C26H18ClN3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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AMPK activator 18
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HY-115549
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