| 中文名称: | ZLN024 | ||||
|---|---|---|---|---|---|
| 英文名称: | ZLN024 | ||||
| 别名: | 2-[2-(2-Bromo-4-methylphenoxy)ethylsulfanyl]pyrimidine | ||||
| CAS No: | 723249-01-2 | 分子式: | C13H13BrN2Os | 分子量: | 325.22 |
| CAS No: | 723249-01-2 | ||||
| 分子式: | C13H13BrN2Os | ||||
| 分子量: | 325.22 | ||||
包装规格：
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
ZLN024 是一种 AMPK 变构激活剂。ZLN024 直接激活重组 AMPK α1β1γ1，AMPK α2β1γ1，AMPK α1β2γ1 和 AMPK α2β2γ1 异源三聚体，EC50 分别为 0.42 μM，0.95 μM，1.1 μM 和 0.13 μM。
溶解性：
溶于DMSO(20mg/mL)
靶点：
AMPK α1β1γ1：0.42 μM (EC50)
AMPK α2β1γ1：0.95 μM (EC50)
AMPK α2β2γ1：0.13 μM (EC50)
AMPK α2β1γ1：0.95 μM (EC50)
AMPK α2β2γ1：0.13 μM (EC50)
体外研究：
ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312). AMPK activation by ZLN024 requires the pre-phosphorylation of Thr-172 by at least one upstream kinase and protects AMPK Thr-172 against dephosphorylation by PP2Cα. ZLN024 activates AMPK in L6 myotubes and stimulates glucose uptake and fatty acid oxidation without increasing the ADP/ATP ratio. Using the established scintillation proximity assay (SPA) assay, random screening against the AMPK α1β1γ1 heterotrimer is performed and a new AMPK activator, ZLN024 is found. ZLN024 directly activates recombinant AMPK α1β1γ1 and its homologue α2β1γ1 in a concentration-dependent manner. ZLN024 increases the activity of α1β1γ1 by 1.5-fold and has an EC50 of 0.42 µM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95 µM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50 of 1.1 µM; and AMPK α2β2γ1, by 1.6-fold with an EC50 of 0.13 µM.
体内研究：
C57BKS db/db mice are administered a 15 mg/kg/day dose of ZLN024 by daily gavage for 5 weeks; 250 mg/kg/day Metformin (Met) is used as a positive control. During the treatment period, there is no significant alteration in food intake and body weight compared with the vehicle group. After 4 weeks of treatment, ZLN024 improves glucose tolerance. ZLN024 reduces the fasting blood glucose by 15%. Liver tissue weight, triacylglycerol and the total cholesterol content are decreased.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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稀释公式
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