CAS NO: | 1883548-91-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | ZLN024 hydrochloride is anAMPKallosteric activator. ZLN024 directly activates recombinantAMPK α1β1γ1,AMPK α2β1γ1,AMPK α1β2γ1andAMPK α2β2γ1heterotrimer withEC50s of 0.42 μM, 0.95 μM, 1.1 μM and 0.13 μM, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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 EC50of 0.42 μM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC50of 0.95 μM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50of 1.1 μM; and AMPK α2β2γ1, by 1.6-fold with an EC50of 0.13 μM[1]. | ||||||||||||||||
体内研究 (In Vivo) | C57BKSdb/dbmice 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[1]. | ||||||||||||||||
分子量 | 361.69 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C13H14BrClN2OS | ||||||||||||||||
CAS 号 | 1883548-91-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 46 mg/mL(127.18 mM) H2O :< 0.1 mg/mL(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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