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Mevastatin

HMG-CoA还原酶抑制剂,Mevastatin (Compactin; ML236B)抑制HMG-CoA还原酶（HMGCR），可抑制类异戊二烯的生物合成，阻断蛋白的异戊二烯化，降低血浆胆固醇水平

目录号: PC12549 纯度: ≥98%

CAS No. :73573-88-3

商品编号	规格	价格	会员价	是否有货	数量
PC12549-50mg	50mg	¥539.00	请登录
PC12549-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称	Mevastatin
中文别名	美伐他汀;美池他汀;美华斯太定;1,3 - 双（2,6 -丙基苯基）咪唑-2-亚基（乙腈）氟硼酸;Mevastatin 美伐他汀;康百汀;康帕丁;美伐他汀技术转让;2-甲基丁酸[1S-[1-Α(R),7-Β,8-Β(2S,4S*),8A-Β]]-1,2,3,7,8,8A-六氢-7-甲基-8-[2-(四氢-4-羟基-6-氧-2H-吡喃-2-基)乙基]-1-萘酯;洛伐他汀杂质A;洛伐他汀杂质A 标准品;辛可芬
英文名称	Mevastatin
英文别名	compactin;Mevastatin;2-Methyl-butanoic acid [1S-[1-alpha(R),7-beta,8-beta(2S,4S*),8a-beta]]-1,2,3,7,8,8a-hexahydro-7-methyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester;ML-236B;[(1S,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-7-methyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate;Mevastatin (Compactin, ML-236B, NSC-281245, CS 500, L 637312, Statin I);MEVASTATIN(SH);(+)-compactin;Antibiotic ML 236B;Compactin (penicillium);Mevastatin (Compactin);Mevastatinum [INN-Latin];ML 236B;Mevastatinum;Mevastatina;Mevastatine;Mevastatin [INN];CS 500;Mevastatine [INN-French];ML 236 B;Mevastatina [INN-Spanish];1UQM1K0W9X;ML236B;7-(1,2,6,7,8,8a-Hexahydro-2-methy
Cas No.	73573-88-3
分子式	C₂₃H₃₄O₅
分子量	390.51
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

性状

Solid

IC50 & Target[1][2]

HMG-CoA reductase
Apoptosis

体外研究(In Vitro)

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.

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

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(In Vivo)

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.

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

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

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

结构分类

Others

来源

Penicillium citrinum

参考文献

[1]. W?chtersh?user A, et al. HMG-CoA reductase inhibitor mevastatin enhances the growth inhibitory effect of butyrate in the colorectal carcinoma cell line Caco-2. Carcinogenesis. 2001 Jul;22(7):1061-7. [Information]

[2]. Amin-Hanjani S, Stagliano NE, Yamada M, et al. Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. Stroke. 2001 Apr;32(4):980-6. [Information]

[3]. Sugazaki M, Hirotani H, Echigo S, et al. Effects of mevastatin on grafted bone in MRL/MpJ mice. Connect Tissue Res. 2010 Apr;51(2):105-12. [Information]

[4]. Evangelopoulos ME, Weis J, Krüttgen A. Mevastatin-induced neurite outgrowth of neuroblastoma cells via activation of EGFR. J Neurosci Res. 2009 Jul;87(9):2138-44. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (640.19 mM; Need ultrasonic)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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