1883548-91-1
物理化学性质
溶解度 | Soluble to 100 mM in DMSO |
形态 | Solid |
颜色 | White to off-white |
ZLN-024 hydrochloride价格(试剂级)
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/11/08 | HY-16708A | ZLN-024 hydrochloride ZLN024 hydrochloride | 1883548-91-1 | 5mg | 540元 |
2024/11/08 | HY-16708A | ZLN-024 hydrochloride ZLN024 hydrochloride | 1883548-91-1 | 10mM * 1mLin DMSO | 594元 |
2024/11/08 | HY-16708A | ZLN-024 hydrochloride ZLN024 hydrochloride | 1883548-91-1 | 10mg | 910元 |
常见问题列表
AMPK α2β2γ1 0.13 μM (EC 50 ) |
AMPK α1β1γ1 0.42 μM (EC 50 ) |
AMPK α2β1γ1 0.95 μM (EC 50 ) |
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 EC 50 of 0.42 µM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC 50 of 0.95 µM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC 50 of 1.1 µM; and AMPK α2β2γ1, by 1.6-fold with an EC 50 of 0.13 µM.
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.