Mevastatin - CAS:73573-88-3

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Mevastatin (Synonyms:美伐他汀; Compactin; ML236B)

目录号 : KM11886 CAS No. : 73573-88-3 纯度 : 98%

Data Sheet 产品使用指南

Mevastatin (Compactin) 是第一个属于他汀类的 HMG-CoA 还原酶抑制剂。Mevastatin 是一种降脂药，可诱导细胞凋亡，将癌细胞阻滞在 G₀/G₁ 期。Mevastatin 还可以增加内皮型一氧化氮合酶 (eNOS) 的 mRNA 和蛋白质水平。Mevastatin 具有抗肿瘤活性，并可用于心血管疾病的研究。

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生物活性

Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G₀/G₁ phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.

体外研究

Mevastatin (0-128 µM; 5 days; Caco-2 cells) treatment causes a dose-dependent decrease in cell number.
Mevastatin (32-128 µM; 24-72 hours; Caco-2 cells) treatment causes an early G0/G1 phase and a late G2/M phase cell cyclr arrest.
Mevastatin (32-128 µM; 72 hours; Caco-2 cells) treatment causes a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1, while cdk 2 and cyclin E protein levels remained unchanged. Cell cycle inhibitors p21 and p27 are significantly upregulated by Mevastatin.
Mevastatin (16-256 µM; Caco-2 cells) treatment induces apoptosis in a dose-dependent manner.
Treatment of Neuro2a cells with mevastatin for 24 hours induced neurite outgrowth associated with up-regulation of the neuronal marker protein NeuN. Mevastatin triggers phosphorylation of the key kinases epidermal growth factor receptor (EGFR), ERK1/2, and Akt/protein kinase B. Inhibition of EGFR, PI3K, and the mitogen-activated protein kinase cascade blocks Mevastatin-induced neurite outgrowth.

Cell Viability Assay

Cell Line:	Caco-2 cells
Concentration:	0 µM, 8 µM, 16 µM, 32 µM, 64 µM, 128 µM
Incubation Time:	5 days
Result:	Caused a dose-dependent decrease in cell number.

Cell Cycle Analysis

Cell Line:	Caco-2 cells
Concentration:	32 µM, 64 µM, 128 µM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Caused a dose-dependent increase of cells in G0/G1 and G2/M phases of the cell cycle.

Western Blot Analysis

Cell Line:	Caco-2 cells
Concentration:	32 µM, 64 µM, 128 µM
Incubation Time:	72 hours
Result:	Resulted in a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1.

体内研究

Mevastatin (2-20 mg/kg; delivered via ALZET miniosmotic pumps; daily; for 7, 14, or 28 days; wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice) treatment increases levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.
The topical infusion of Mevastatin (2.5 pmol/hr) increases bone mass (MRL/MpJ mouse) of isografted bone by increasing bone turnover and, at least in part, by promoting the expression of bone morphogenetic protein-2 (BMP-2) mRNA and receptor activator of NF-κB ligand (RANKL) mRNA.

Animal Model:	Wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice (18-22 g) with the filament model
Dosage:	2 mg/kg or 20 mg/kg
Administration:	Delivered via 7- or 14-day ALZET miniosmotic pumps implanted subcutaneously; daily; for 7, 14, or 28 days
Result:	Increased levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduced infarct size, and improved neurological deficits in a dose- and time-dependent manner.

分子式

C₂₃H₃₄O₅

分子量

390.51

CAS号

73573-88-3

中文名称

美伐他汀；康百汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

In Vitro:

DMSO : : 200 mg/mL (512.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5608 mL	12.8038 mL	25.6075 mL
5 mM	0.5122 mL	2.5608 mL	5.1215 mL
10 mM	0.2561 mL	1.2804 mL	2.5608 mL

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)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 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 μL 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% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 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。

科研文献

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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