Mevastatin (Synonyms: 美伐他汀; Compactin; ML236B)
Mevastatin (Compactin) 是屬于他汀類的 HMG-CoA 還原酶抑制劑。Mevastatin 是一種降脂藥，可誘導(dǎo)細(xì)胞凋亡，將癌細(xì)胞阻滯在 G0/G1 期。Mevastatin 還可以增加內(nèi)皮型一氧化氮合酶 (eNOS) 的 mRNA 和蛋白質(zhì)水平。Mevastatin 具有抗腫瘤活性，并可用于心血管疾病的研究。
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[1][2][3].
IC50 & Target
HMG-CoA reductase[1][2]
Apoptosis[1]
體外研究(In Vitro)
Mevastatin (0-128 µM; 5 days; Caco-2 cells) treatment causes a dose-dependent decrease in cell number[1].
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[1].
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[1].
Mevastatin (16-256 µM; Caco-2 cells) treatment induces apoptosis in a dose-dependent manner[1].
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[4].
Cell Viability Assay[2]
| 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. |
體內(nèi)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[2].
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[3].
| Animal Model: | Wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice (18-22 g) with the filament model[2] |
| 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. |
分子量：390.51
性狀：Solid
Formula：C23H34O5
CAS 號：73573-88-3
中文名稱：洛伐ta汀EP雜質(zhì)A
來源：Penicillium citrinum
運(yùn)輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
DMSO : 250 mg/mL (640.19 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
參考文獻(xiàn)
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
注：產(chǎn)品僅用于科研
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