ZLN-024 hydrochloride
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- CAS号:
- 1883548-91-1
- 英文名:
- ZLN-024 hydrochloride
- 英文别名:
- ZLN024 hydrochloride;ZLN-024 hydrochloride;Inhibitor,AMP-activated protein kinase,ZLN-024,ZLN 024 hydrochloride,inhibit,ZLN024,ZLN 024,AMPK
- 中文名:
- ZLN-024 hydrochloride
- 中文别名:
- ZLN024盐酸盐;化合物ZLN 024 HYDROCHLORIDE;2-((2-(2-溴-4-甲基苯氧基)乙基)硫基)嘧啶盐酸盐
- CBNumber:
- CB52729380
- 分子式:
- C13H14BrClN2OS
- 分子量:
- 361.68
- MOL File:
- 1883548-91-1.mol
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ZLN-024 hydrochloride化学性质
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溶解度:
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Soluble to 100 mM in DMSO
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形态:
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Solid
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颜色:
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White to off-white
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ZLN-024 hydrochloride性质、用途与生产工艺
ZLN024 hydrochloride 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。
AMPK α2β2γ1
0.13 μM (EC
50
)
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AMPK α1β1γ1
0.42 μM (EC
50
)
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AMPK α2β1γ1
0.95 μM (EC
50
)
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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.
ZLN-024 hydrochloride
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-16708A | ZLN-024 hydrochloride ZLN024 hydrochloride | 1883548-91-1 | 5mg | 540元 |
2024/04/30 | HY-16708A | ZLN-024 hydrochloride ZLN024 hydrochloride | 1883548-91-1 | 10mM * 1mLin DMSO | 594元 |
ZLN-024 hydrochloride
生产厂家
1883548-91-1, ZLN-024 hydrochloride 相关搜索:
- CHBrClNOS
- 2-((2-(2-溴-4-甲基苯氧基)乙基)硫基)嘧啶盐酸盐
- 化合物ZLN 024 HYDROCHLORIDE
- ZLN024盐酸盐
- 1883548-91-1
- Inhibitor,AMP-activated protein kinase,ZLN-024,ZLN 024 hydrochloride,inhibit,ZLN024,ZLN 024,AMPK
- ZLN-024 hydrochloride
- ZLN024 hydrochloride