1. Metabolic Enzyme/Protease Apoptosis
  2. HMG-CoA Reductase (HMGCR) Ferroptosis
  3. Cerivastatin sodium

Cerivastatin sodium  (Synonyms: 西立伐他汀钠)

目录号: HY-109523 纯度: 99.84%
COA 产品使用指南

Cerivastatin sodium 是一种合成的降脂剂,是一种高效,耐受性好,口服活性的 HMG-CoA 还原酶抑制剂,Ki 为 1.3 nM/L。Cerivastatin sodium 可降低低密度脂蛋白胆固醇水平。Cerivastatin sodium 还主要通过 RhoA 抑制作用来抑制 MDA-MB-231 细胞的增殖和侵袭,具有抗癌作用。

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Cerivastatin sodium Chemical Structure

Cerivastatin sodium Chemical Structure

CAS No. : 143201-11-0

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10 mM * 1 mL in Water ¥1540
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1 mg ¥636
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5 mg ¥1400
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Customer Review

Other Forms of Cerivastatin sodium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2].

IC50 & Target

Ki: 1.3 nM/L (HMG-CoA reductase)[1][2][3]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Hepatocyte IC50
1.7 nM
Compound: cer, cerivastatin
Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
[PMID: 17560788]
HepG2 IC50
0.13 μM
Compound: Cerivastatin
Cytotoxicity against human HepG2 cells assessed as reduction in nuclear size after 72 hrs by fluorescent image analysis
Cytotoxicity against human HepG2 cells assessed as reduction in nuclear size after 72 hrs by fluorescent image analysis
[PMID: 27105029]
HepG2 IC50
0.34 μM
Compound: Cerivastatin
Cytotoxicity against human HepG2 cells assessed as increase in intracellular free calcium level after 72 hrs by fluorescent image analysis
Cytotoxicity against human HepG2 cells assessed as increase in intracellular free calcium level after 72 hrs by fluorescent image analysis
[PMID: 27105029]
HepG2 IC50
0.6 μM
Compound: Cerivastatin
Cytotoxicity against human HepG2 cells assessed as reduction in mitochondrial membrane potential after 72 hrs by fluorescent image analysis
Cytotoxicity against human HepG2 cells assessed as reduction in mitochondrial membrane potential after 72 hrs by fluorescent image analysis
[PMID: 27105029]
HepG2 IC50
0.8 μM
Compound: Cerivastatin
Cytotoxicity against human HepG2 cells assessed as increase in membrane permeability after 72 hrs by fluorescent image analysis
Cytotoxicity against human HepG2 cells assessed as increase in membrane permeability after 72 hrs by fluorescent image analysis
[PMID: 27105029]
HepG2 IC50
0.96 μM
Compound: Cerivastatin
Cytotoxicity against human HepG2 cells assessed as reduction in cell number after 72 hrs by fluorescent image analysis
Cytotoxicity against human HepG2 cells assessed as reduction in cell number after 72 hrs by fluorescent image analysis
[PMID: 27105029]
L6 IC50
7 nM
Compound: cer, cerivastatin
Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
[PMID: 17560788]
体外研究
(In Vitro)

Cerivastatin sodium (5-50 ng/mL;3 天;MDA-MB-231 细胞) 处理诱导 MDA-MB-231 细胞增殖的剂量依赖性降低 (在 25 ng/mL 时抑制高达 40%)[1]
Cerivastatin sodium (25 ng/mL;18-36 小时;MDA-MB-231 细胞) 处理 36 小时后诱导细胞周期停滞在 G 1/S 期.较短的孵育时间 (18 小时) 未观察到这种停滞[1]
Cerivastatin sodium (25 ng/mL;18 小时;MDA-MB-231 细胞) 处理诱导显著的 p21Waf1/Cip1 水平增加[1]
Cerivastatin sodium (25 ng/mL;12 小时;MDA-MB-231 细胞) 处理增加MDA-MB-231 细胞中的 p21 转录本[1]
Cerivastatin sodium (10-25 ng/mL;18 小时) 通过 Matrigel 抑制 MDA-MB-231 细胞的侵袭[1]
Cerivastatin sodium (25 ng/mL;18-36 小时) 使 RhoA 和 Ras 从细胞膜离域到胞质溶胶并诱导形态学变化[1]
Cerivastatin sodium (25 ng/mL;4-36 小时) 以 RhoA 抑制依赖性方式诱导 NFκB 失活,导致尿激酶和金属蛋白酶 9 表达降低,同时增加 IκB[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 5 ng/mL, 10 ng/mL, 25 ng/mL, 50 ng/mL
Incubation Time: 3 days
Result: Induced a dose-dependent decrease in cell proliferation of MDA-MB-231 cells.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 25 ng/mL
Incubation Time: 18 hours, 36 hours
Result: Induced a cell cycle block in G 1/S phase.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 25 ng/mL
Incubation Time: 18 hours
Result: Induced a marked increase in the level of p21Waf1/Cip1.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 25 ng/mL
Incubation Time: 12 hours
Result: Increased p21Waf1/Cip1 mRNA levels.
体内研究
(In Vivo)

Cerivastatin sodium 吸收良好,在口服给药后 1-3 小时内达到最大血浆浓度。在循环中,Cerivastatin sodium 与血浆蛋白高度结合 (99.5%),消除半衰期为 2-4 小时。Cerivastatin sodium 主要在肝脏中代谢为三种极性代谢物。其中两种代谢物具有活性,但与母体药物相比程度较小,第三种代谢物无活性。所有代谢物的血浆浓度都大大低于母体药物的血浆浓度。代谢物通过尿液 (20-25%) 和粪便 (66-73%) 消除,而基本上没有母体化合物排出[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

481.53

Formula

C26H33FNNaO5

CAS 号
性状

固体

颜色

White to off-white

中文名称

西立伐他汀钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 100 mg/mL (207.67 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : 50 mg/mL (103.84 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0767 mL 10.3836 mL 20.7671 mL
5 mM 0.4153 mL 2.0767 mL 4.1534 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.89%

参考文献

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.0767 mL 10.3836 mL 20.7671 mL 51.9178 mL
5 mM 0.4153 mL 2.0767 mL 4.1534 mL 10.3836 mL
10 mM 0.2077 mL 1.0384 mL 2.0767 mL 5.1918 mL
15 mM 0.1384 mL 0.6922 mL 1.3845 mL 3.4612 mL
20 mM 0.1038 mL 0.5192 mL 1.0384 mL 2.5959 mL
25 mM 0.0831 mL 0.4153 mL 0.8307 mL 2.0767 mL
30 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7306 mL
40 mM 0.0519 mL 0.2596 mL 0.5192 mL 1.2979 mL
50 mM 0.0415 mL 0.2077 mL 0.4153 mL 1.0384 mL
60 mM 0.0346 mL 0.1731 mL 0.3461 mL 0.8653 mL
80 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6490 mL
100 mM 0.0208 mL 0.1038 mL 0.2077 mL 0.5192 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Cerivastatin sodium
目录号:
HY-109523
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