ZLN024 hydrochloride - CAS:1883548-91-1 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	ZLN024 hydrochloride
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

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

Z10047 ZLN024 hydrochloride ≥98% (psaitong)

相关产品

包装规格：

5mg 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℃

UN码：

HazardClass：

危害声明：

安全说明：

搜索质检报告(COA)

参考文献 & 客户发表文献

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

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

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 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果