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（ 母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们客服联系。| 中文名称: | ZLN024 hydrochloride 一键复制产品信息 | ||||
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| 英文名称: | ZLN024 hydrochloride | ||||
| 别名: | 2-[[2-(2-Bromo-4-methylphenoxy)ethyl]thio]pyrimidine hydrochloride;ZLN 024 hydrochloride;ZLN024 (hydrochloride);ZLN024 hydrochloride | ||||
| CAS No: | 1883548-91-1 | 分子式: | C13H14BrClN2Os | 分子量: | 361.69 |
| CAS No: | 1883548-91-1 | ||||
| 分子式: | C13H14BrClN2Os | ||||
| 分子量: | 361.69 | ||||
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
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产品编号：Z10047 |
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产品名称：ZLN024 hydrochloride |
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CAS: |
1883548-91-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
361.69 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.7648mL |
13.8240mL |
27.6480mL |
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5mM |
0.5530mL |
2.7648mL |
5.5296mL |
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10mM |
0.2765mL |
1.3824mL |
2.7648mL |
生物活性
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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。 |
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靶点/IC50 |
AMPK α2β2γ1 0.13μM (EC50) |
AMPK α1β1γ1 0.42μM (EC50) |
AMPK α2β1γ1 |
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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. |
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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. |
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推荐实验方法(仅供参考)
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激酶实验： |
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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. |
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动物实验: |
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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. |
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保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
(2).jpg)
体内配方的制备方法: 取 50μLDMSO 母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清
方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL Saline/PBS/ddH2O，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
