Fluvastatin
(Synonyms: 氟伐他汀; XU 62-320 free acid) 目录号 : GC13535
Fluvastatin是一种亲脂性的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，可在多种癌细胞中抑制增殖并诱导凋亡。
Cas No.:93957-54-1
Sample solution is provided at 25 µL, 10mM.
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Fluvastatin, a lipophilic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, suppresses proliferation and induces apoptosis in various cancer cells[1-2]. Fluvastatin, which structurally mimics HMG-CoA to competitively block the enzyme’s active site, lowers total and low-density lipoprotein (LDL) cholesterol while exerting anti-atherogenic, antithrombotic, and antioxidant effects and improving vascular function[2-3].
In vitro, after 72h of treatment with the increasing concentrations of Fluvastatin (5, 10, and 20μM), human endometrial cancer (EC) cells exhibited a concentration-dependent decline in viability and proliferation, markedly reduced migration and invasion, and elevated apoptosis accompanied by progressive up-regulation of p53 and cleaved caspase-3[4]. A 24h incubation with 2.5μM Fluvastatin reproducibly gave over 50% inhibition of thrombin-induced von Willebrand factor (vWF) secretion, was more effective than shorter incubation times, did not disrupt the human umbilical-vein endothelial cells (HUVEC) culture monolayer, and did not change vWF antigen levels measured in cell lysates[5].
In vivo, after four daily intraperitoneal injections of 10mg/kg Fluvastatin in female C57BL/6J mice, total peritoneal cell counts remained unchanged, yet the proportion and absolute number of mast cells recovered from peritoneal lavage were markedly reduced[6]. The rats treated by gavage with 10mg/kg Fluvastatin showed a reduced number of polymorphonuclear neutrophils (PMN) compared to the control rats at 4h postinjection[7].
References:
[1] Zhang W, Wu J, Zhou L, et al. Fluvastatin, a lipophilic statin, induces apoptosis in human hepatocellular carcinoma cells through mitochondria-operated pathway. Indian J Exp Biol. 2010;48(12):1167-1174.
[2] Langtry HD, Markham A. Fluvastatin: a review of its use in lipid disorders. Drugs. 1999;57(4):583-606.
[3] Bonds M, Bordoni B. Fluvastatin. In: StatPearls. StatPearls Publishing; 2023.
[4] Cai Y, Zhao F. Fluvastatin suppresses the proliferation, invasion, and migration and promotes the apoptosis of endometrial cancer cells by upregulating Sirtuin 6 (SIRT6). Bioengineered. 2021;12(2):12509-12520.
[5] Fish RJ, Yang H, Viglino C, et al. Fluvastatin inhibits regulated secretion of endothelial cell von Willebrand factor in response to diverse secretagogues. Biochem J. 2007;405(3):597-604.
[6] Paez PA, Kolawole M, Taruselli MT, et al. Fluvastatin Induces Apoptosis in Primary and Transformed Mast Cells. J Pharmacol Exp Ther. 2020;374(1):104-112.
[7] Fischetti F, Carretta R, Borotto G, et al. Fluvastatin treatment inhibits leucocyte adhesion and extravasation in models of complement-mediated acute inflammation. Clin Exp Immunol. 2004;135(2):186-193.
Fluvastatin是一种亲脂性的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，可在多种癌细胞中抑制增殖并诱导凋亡[1-2]。Fluvastatin分子结构模拟HMG-CoA，通过竞争性占据酶的活性位点，降低总胆固醇和低密度脂蛋白（LDL）胆固醇水平，同时发挥抗动脉粥样硬化、抗血栓及抗氧化作用，并改善血管功能[2-3]。
在体外，对人子宫内膜癌（EC）细胞给予5、10和20μM递增浓度的Fluvastatin处理72小时后，细胞的存活率和增殖能力呈浓度依赖性下降，迁移和侵袭能力显著削弱，细胞凋亡水平升高，且p53和剪切型caspase-3表达逐步上调[4]。将人脐静脉内皮细胞（HUVEC）与2.5μM的Fluvastatin共孵育24小时，可稳定地抑制凝血酶诱导的血管性血友病因子（vWF）分泌超过50%，抑制效果优于更短孵育时间，且既不破坏HUVEC单层结构，也不改变细胞裂解液中的vWF抗原水平[5]。
在体内，对雌C57BL/6J小鼠连续4天腹腔注射10mg/kg的Fluvastatin后，腹腔总细胞数未见变化，但灌洗液中肥大细胞的比例和绝对数量均显著减少[6]。经灌胃给予10mg/kg的Fluvastatin大鼠，在注射后4小时，其多形核中性粒细胞（PMN）数量较对照组显著下降[7]。
| Cell experiment [1]: | |
Cell lines | Human endometrial cancer (EC) cell lines (RL95-2 and KLE) |
Preparation Method | Cells were maintained at 37°C with 5% CO2 and cultivated in DMEM containing 10% FBS. 48h later, Fluvastatin with different concentrations (5, 10, 20μM) was employed to incubate cells for 72h for the following experiments. |
Reaction Conditions | 5, 10, 20μM; 72h |
Applications | Fluvastatin inhibited the viability and proliferation of KLE and RL95-2 endometrial cancer cells in a concentration-dependent manner, while markedly suppressing their migratory and invasive capacities. Fluvastatin dose-dependently triggered apoptosis in KLE and RL95-2 cells, accompanied by progressive increases in p53 and cleaved caspase-3 levels. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Female C57BL/6J mice received 10mg/kg Fluvastatin or vehicle (DMSO diluted in PBS to match Fluvastatin solvent) daily by intraperitoneal injection for 4 days. Mice were sacrificed, and peritoneal lavage was harvested and analyzed for mast cells by staining for CD45+ cells and gating on FcεRI+/c-Kit+ cells. Cross sections of the small intestine were also analyzed by histology, using staining with pinacyanol erythosinate to identify mast cells. |
Dosage form | 10mg/kg; intraperitoneal injection |
Applications | Fluvastatin did not reduce total peritoneal cells but greatly reduced the proportion and total number of mast cells found in peritoneal lavage. |
References: | |
| Cas No. | 93957-54-1 | SDF | |
| 别名 | 氟伐他汀; XU 62-320 free acid | ||
| 化学名 | (E,3R,5S)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoic acid | ||
| Canonical SMILES | CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)O)O)O)C3=CC=C(C=C3)F | ||
| 分子式 | C24H26FNO4 | 分子量 | 411.47 |
| 溶解度 | ≥ 20.57 mg/mL in DMSO, ≥ 42.2 mg/mL in EtOH with gentle warming, ≥ 32.53 mg/mL in Water with gentle warming | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4303 mL | 12.1516 mL | 24.3031 mL |
| 5 mM | 0.4861 mL | 2.4303 mL | 4.8606 mL |
| 10 mM | 0.243 mL | 1.2152 mL | 2.4303 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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