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

Cerivastatin sodium  (Synonyms: 西立伐他汀鈉)

目錄號(hào): HY-109523 純度: 99.84%
COA 產(chǎn)品使用指南 技術(shù)支持

Cerivastatin sodium 是一種合成的降脂劑,是一種高效,耐受性好,口服活性的 HMG-CoA 還原酶抑制劑,Ki 為 1.3 nM/L。Cerivastatin sodium 可降低低密度脂蛋白膽固醇水平。Cerivastatin sodium 還主要通過(guò) RhoA 抑制作用來(lái)抑制 MDA-MB-231 細(xì)胞的增殖和侵襲,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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Other Forms of Cerivastatin sodium:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

細(xì)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]
體外研究
(In Vitro)

Cerivastatin sodium (5-50 ng/mL;3 天;MDA-MB-231 細(xì)胞) 處理誘導(dǎo) MDA-MB-231 細(xì)胞增殖的劑量依賴性降低 (在 25 ng/mL 時(shí)抑制高達(dá) 40%)[1]。
Cerivastatin sodium (25 ng/mL;18-36 小時(shí);MDA-MB-231 細(xì)胞) 處理 36 小時(shí)后誘導(dǎo)細(xì)胞周期停滯在 G 1/S 期.較短的孵育時(shí)間 (18 小時(shí)) 未觀察到這種停滯[1]。
Cerivastatin sodium (25 ng/mL;18 小時(shí);MDA-MB-231 細(xì)胞) 處理誘導(dǎo)顯著的 p21Waf1/Cip1 水平增加[1]
Cerivastatin sodium (25 ng/mL;12 小時(shí);MDA-MB-231 細(xì)胞) 處理增加MDA-MB-231 細(xì)胞中的 p21 轉(zhuǎn)錄本[1]。
Cerivastatin sodium (10-25 ng/mL;18 小時(shí)) 通過(guò) Matrigel 抑制 MDA-MB-231 細(xì)胞的侵襲[1]。
Cerivastatin sodium (25 ng/mL;18-36 小時(shí)) 使 RhoA 和 Ras 從細(xì)胞膜離域到胞質(zhì)溶膠并誘導(dǎo)形態(tài)學(xué)變化[1]。
Cerivastatin sodium (25 ng/mL;4-36 小時(shí)) 以 RhoA 抑制依賴性方式誘導(dǎo) NFκB 失活,導(dǎo)致尿激酶和金屬蛋白酶 9 表達(dá)降低,同時(shí)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.
體內(nèi)研究
(In Vivo)

Cerivastatin sodium 吸收良好,在口服給藥后 1-3 小時(shí)內(nèi)達(dá)到最大血漿濃度。在循環(huán)中,Cerivastatin sodium 與血漿蛋白高度結(jié)合 (99.5%),消除半衰期為 2-4 小時(shí)。Cerivastatin sodium 主要在肝臟中代謝為三種極性代謝物。其中兩種代謝物具有活性,但與母體藥物相比程度較小,第三種代謝物無(wú)活性。所有代謝物的血漿濃度都大大低于母體藥物的血漿濃度。代謝物通過(guò)尿液 (20-25%) 和糞便 (66-73%) 消除,而基本上沒(méi)有母體化合物排出[2]。

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

分子量

481.53

Formula

C26H33FNNaO5

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

西立伐他汀鈉

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

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

DMSO 中的溶解度 : 50 mg/mL (103.84 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備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儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.89%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備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儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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  • 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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Cerivastatin sodium
目錄號(hào):
HY-109523
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