依折麦布 - CAS:163222-33-1 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	依折麦布促销
英文名称:	Ezetimibe
别名:	依泽替米贝 Ezetimibe
CAS No:	163222-33-1	分子式:	C₂₄H₂₁F₂NO₃	分子量:	409.43
CAS No:	163222-33-1
分子式:	C₂₄H₂₁F₂NO₃
分子量:	409.43
MDL:	MFCD00937872

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E10004 依折麦布 99% (psaitong)

相关产品

熔点：

162-164℃

外观与性状：

白色结晶性粉末

包装规格：

100mg 1g 5g in glass bottle

溶解性：

溶于DMSO（82mg/ml）、乙醇（82mg/ml)和甲醇

产品描述：

基本信息

产品编号：	E10004
产品名称：	Ezetimibe
CAS:	163222-33-1	储存条件	粉末	2-8℃	四年

分子式：	C24H21F2NO3		溶于液体	-80℃	6个月
分子量：	409.43			-20℃	1个月
化学名：	(3R,4S)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one
Solubility (25°C)：
体外:	DMSO	82mg/mL (200.29mM)
	Ethanol	82mg/mL (200.29mM)
	Water	Insoluble
体内(现配现用):	1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(6.11mM);Clear solution
	此⽅案可获得 ≥ 2.5 mg/mL (6.11 mM，饱和度未知) 的澄清溶液。以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μ L Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。
	2.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(6.11mM);Clear solution
	此⽅案可获得 ≥ 2.5 mg/mL (6.11 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。
＜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	2.4426mL	12.2130mL	24.4260mL
5mM	0.4885mL	2.4426mL	4.8852mL
10mM	0.2443mL	1.2213mL	2.4426mL

生物活性

产品描述	一种NPC1L1抑制剂。
靶点	NPC1L1,Nrf2
体外研究	Ezetimibe (Eze) acts as a potent Nrf2 activator without causing cytotoxicity.Ezetimibe enhances transactivation of Nrf2,as revealed by a luciferase reporter assay.Ezetimibe also upregulates Nrf2 target genes, including GSTA1,heme oxygenase-1 (HO-1) and Nqo-1 in Hepa1c1c7 and MEF cells.Ezetimibe upregulates Nrf2 target genes in Nrf2+/+MEF cells,whereas this induction is totally blocked in Nrf2-/-MEF cells.Taken together,Ezetimibe acts as a novel Nrf2 inducer in a ROS-independent manner.Human huh7 hepatocytes are pretreated with Ezetimibe (10μM,1h) and incubated with palmitic acid (PA,0.5mM,24h) to induce hepatic steatosis.Ezetimibe treatment significantly attenuates PA-increased triglycerides (TG) levels,which is consistent with our animal study.PA treatment resulted in an approximately 20% decrease in mRNA expression of ATG5,ATG6,and ATG7,which had been increased by Ezetimibe treatment.In addition,Ezetimibe treatment significantly increased the PA-induced reduction in LC3 protein abundance.
体内研究	Administration of Ezetimibe (Eze) reduces the liver weights of mice fed the methionine- and choline-deficient (MCD) diet.This is consistent with the beneficial effects of Ezetimibe on hepatic steatosis.Liver histology shows pronounced multiple macrovesicular fat droplets in mice on the MCD diet,but Ezetimibe treatment markedly decreases the number and size of those droplets.Furthermore,hepatic fibrosis in mice fed the MCD diet is significantly attenuated by Ezetimibe.Blood and liver lipid levels including TG,free fatty acids (FFA),and total cholesterol (TC) are significantly decreased in Ezetimibetreated OLETF rats.Moreover,OLETF rats show higher serum levels of glucose,insulin,HOMA-IR,TG,FFA,and TC than LETF animals,which are significantly reduced by Ezetimibe.In addition,histological analysis indicated that OLETF control rats showed larger lipid droplets in hepatocytes than age-matched LETO controls,which are attenuated by administration of Ezetimibe.

推荐实验方法(仅供参考)

激酶实验：

GST-p62 is prepared from Escherichia coli and 0.5μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay.Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP.AMPK complex is immuno-purified from the HEK293 cells,to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD,D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20mM HEPES,pH7.4,1mM EGTA, 0.4mM EDTA,5mM MgCl2,0.05mM DTT,0.5μg GST-p62,0.2mM AMP,and 1mM ATPγS.Reaction is carried out at 37℃ for 30 min,and then terminated by adding 20mM EDTA.To detect γSlabeled p62 protein,the reaction product is alkylated with 2.5mM PNBM for 2h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody.

细胞实验:
Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS,100 units/mL penicillin and 100μg/mL streptomycin at 37℃ in a 95% air/5% CO2 atmosphere.Hepatocytes are treated with or without Ezetimibe (10μM,1h) and incubated with palmitic acid (PA,0.5mM,24h).

动物实验:

Mice

Ten-week-old C57BL/6J male mice are used.These animals are randomly assigned to one of three groups (7-10 mice in each group):normal chow diet;MCD diet,vehicle-treated;or MCD diet,Ezetimibe -treated.The mice had free access to diet and water,with temperature maintained at 23±2℃,humidity of 60%±10%,and 12-h light/dark cycles.In the MCD diet with Ezetimibe group,Ezetimibe 10mg/kg is given once daily by oral gavage for 4 weeks.The chow and MCD diet with vehicle groups received the same volume of phosphate buffered saline orally for 4 weeks.Body weight is measured once a week over the course of the treatment period.After 4 weeks,the mice are anesthetized and killed;blood is collected via heart puncture.Tissues are harvested and either snap-frozen in liquid nitrogen and stored at −70℃ or fixed in formalin and embedded in paraffin.

Rats

Male OLETF (n=11) and age-matched LETO rats (n=3) are used, and experiments are conducted in a specific pathogen-free facility with a 12h light/dark cycle.The OLETF rat is a model that represents late-onset hyperglycemia and exhibits a chronic disease course,mild obesity and clinical onset of diabetes mellitus.Animals have unrestricted access to water and food.At 12 wk of age,rats are randomized and treated with either PBS or Ezetimibe (10mg/kg per day) via a stomach gavage for 20 wk.At the end of the study,the rats are fasted overnight and anesthetized with intraperitoneal Zoletil/Rompun.Blood is collected from the abdominal aorta,and liver tissues are dissected,immediately frozen in liquid nitrogen,and stored at -80℃ until further analysis.

保存条件：

2-8℃

UN码：

HazardClass：

危害声明：

安全说明：

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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