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ZLN024 hydrochloride  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥46mg/mL）
产品描述：基本信息 产品编号：Z10047 产品名称：ZLN024 hydrochloride CAS: 1883548-91-1   储存条件 粉末 -20℃ 四年     分子式： C13H14BrClN2Os 溶于液体 -80℃ 六个月 分子量： 361.69 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7648mL 13.8240mL 27.6480mL 5mM 0.5530mL 2.7648mL 5.5296mL 10mM 0.2765mL 1.3824mL 2.7648mL   生物活性 产品描述 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 0.42μM，0.95μM，1.1μM 和 0.13μM。 靶点/IC50 AMPK α2β2γ1 0.13μM (EC50) AMPK α1β1γ1 0.42μM (EC50) AMPK α2β1γ1 0.95μM (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 0.42µM,and it increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95µM.ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50 of 1.1µM;and AMPK α2β2γ1, by 1.6-fold with an EC50 of 0.13µM. 体内研究 C57BKS db/db mice are administered a 15mg/kg/day dose of ZLN024 by daily gavage for 5 weeks;250mg/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.   推荐实验方法(仅供参考) 激酶实验： Before the scintillation proximity assay (SPA) assay,200nM recombinant AMPK protein (α1β1γ1,α2β1γ1,α1β2γ1,α2β2γ1,α1(1-394),α1(1-335),α1(1-312)) is constructed,expressed,purified and fully phosphorylated.The SPA reactions are performed in 96-well plates in a final volume of 50µL containing 20mM Tris-HCl,pH 7.5,5mM MgCl2,1mM DTT,2µM biotinSAMS,2µM ATP and 7.4×103 Bq/well [γ-33P]ATP. The reactions are initiated by the addition of 50nM recombinant AMPK protein to the reaction solutions,followed by incubation at 30℃ for 2hr.The reactions are then terminated by the addition of 40µL of stop solution containing 80µg Streptavidin-coated SPA beads per well,50mM EDTA and 0.1% Triton X-100 in PBS,pH 7.5,followed by incubation for 1hr.Finally,160µL of suspension solution containing 2.4M CsCl,50mM EDTA and 0.1% Triton X-100 in PBS,pH 7.5,is added to the reaction solution to suspend the SPA beads completely.The SPA signals are measured in a Wallac Microbeta plate counter 30 min later.   动物实验:   Mice C57BKS db/db mice are maintained under a 12 hr light-dark cycle with free access to water and food.At 8 weeks of age,male db/db mice are randomly assigned to the various treatment groups by body weight and glucose levels (n=6-8).The treatment groups for the 5-week chronic study are as follows:vehicle (0.5% methylcellulose),ZLN024 (15mg/kg) and Metformin (250mg/kg).The treatments are orally administered once daily.The body weights and food intake are measured daily.After 5 weeks of treatment,the mice are killed after a final dose,and the tissues are collected for further analysis.
保存条件：-20℃

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