Lovastatin
(Synonyms: 洛伐他汀; Mevinolin) 目录号 : GC11633An inhibitor of HMG-CoA reductase
Cas No.:75330-75-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
HeLa, MCF-7 and HepG2 cell lines |
Preparation method |
The solubility of this compound in DMSO is >20.2 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
5-1600 μg/ml |
Applications |
Lovastatin, other than its anticholesterol property, has diverse applications in the field of osteoporosis, neuro-degeneration, rheumatoid arthritis, antifungals and also is reported to reduce proliferation of lung cancer cells, breast cancer (MCF-7), liver cancer (HepG2). Lovastatin treatments show significant dose dependent cytotoxic effect on HeLa cells with IC50 value of 160 μg/mL. |
Animal experiment [2]: | |
Animal models |
guinea pig wound chamber model |
Dosage form |
5 microM for 8 d |
Application |
The ability of lovastatin to induce fibroblast apoptosis in vivo was examined using a guinea pig wound chamber model. Lovastatin (5 microM, 8 d) reduced granulation tissue formation in the wound chambers by 64.7%, with associated ultrastructural evidence of fibroblast apoptosis. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Bhargavi S, et al. Purification of Lovastatin from Aspergillus terreus (KM017963) and Evaluation of its Anticancer and Antioxidant Properties. Asian Pac J Cancer Prev. 2016;17(8):3797-803. [2] Tobert JA, et al. Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. |
Lovastatin is an inhibitor of 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase with IC50 values of 2.3 nmol/L in rat liver cells and 5 nmol/L in the human liver hepatocellular carcinoma cell line, HepG2 [1].
HMG-CoA reductase is responsible for the catalysis of the rate-limiting step in the biosynthesis of cholesterol. It catalyzes the conversion of HMG-CoA to mevalonate, the second step in the production of cholesterol in cells [2].
Lovastatin prevented the proliferation of several cell types by inhibiting the production of mevalonate and its metabolites. Inhibition of mevalonate formation also prevented the production of isoprenoids which are necessary for cell proliferation and other important cell functions. This reduction in isoprenoids caused beneficial pleiotropic effects. Lovastatin caused reduction in DNA synthesis at concentrations of 1 to 20 µM. At 1 µM, it inhibited the increase of mesangial cells in culture. Lovastatin (5 μM) also increased efferocytosis (phagocytosis of apoptotic cells) after 6 hours. However, after 24 hours, its effect was dose-dependent, with a maximum at 10 µM [3, 4, 5].
Mice treated with lovastatin (10 mg/kg) three times over 30 hours showed increased efferocytosis by alveolar macrophages. In a guinea pig wound chamber model, lovastatin (5 µM, 8 days) decreased granulation tissue formation by 64.7% [5, 6].
References:
[1]. Amin D, Gustafson SK, Weinacht JM, et al. RG 12561 (Dalvastatin): A novel synthetic inhibitor of HMG-CoA reductase and cholesterol-lowering agent. Pharmacology, 1993, 46(1): 13-22.
[2]. Tobert JA. Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nature Reviews Drug Discovery, 2003, 2(7): 517-526.
[3]. Massy ZA, Keane WF, Kasiske BL. Inhibition of the mevalonate pathway: benefits beyond cholesterol reduction. The Lancet, 1996, 347(8994): 102-103.
[4]. O'Donnell MP, Kasiske BL, Kim Y, et al. Lovastatin inhibits proliferation of rat mesangial cells. Journal of Clinical Investigation, 1993, 91(1): 83.
[5]. Morimoto K, Janssen WJ, Fessler MB, et al. Lovastatin enhances clearance of apoptotic cells (efferocytosis) with implications for chronic obstructive pulmonary disease. The Journal of Immunology, 2006, 176(12): 7657-7665.
[6]. Tan A, Levrey H, Dahm C, et al. Lovastatin induces fibroblast apoptosis in vitro and in vivo: a possible therapy for fibroproliferative disorders. American journal of respiratory and critical care medicine, 1999, 159(1): 220-227.
Cas No. | 75330-75-5 | SDF | |
别名 | 洛伐他汀; Mevinolin | ||
化学名 | [(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate | ||
Canonical SMILES | CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C | ||
分子式 | C24H36O5 | 分子量 | 404.54 |
溶解度 | ≥ 20.2 mg/mL in DMSO, ≥ 18.6 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4719 mL | 12.3597 mL | 24.7194 mL |
5 mM | 0.4944 mL | 2.4719 mL | 4.9439 mL |
10 mM | 0.2472 mL | 1.236 mL | 2.4719 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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