Lovastatin
(Synonyms: 洛伐他汀; Mevinolin) 目录号 : GC11633
Lovastatin是一种3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，通过影响甲羟戊酸途径来发挥作用，IC50值为77nM。
Cas No.:75330-75-5
Sample solution is provided at 25 µL, 10mM.
Lovastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that impacts the mevalonate pathway[1], which has an IC50 value of 77nM[2]. Lovastatin can inhibit cholesterol synthesis[3], EC50 value is 0.002mg/kg[2].
Lovastatin can induce apoptosis (10μM , 24h) inspontaneously immortalized rat brain neuroblasts[4]. Lovastatin efficiently inhibited Ras activation,which was associated with a significant decrease in ERK1/2 (extracellular-signalregulated kinase1/2) phosphorylation[4] . Lovastatin can inhibit A549 (human lung adenocarcinoma cells) cell proliferation (50μM , 24h) by regulating the ERK1/2 and COX-2 pathways[5].
Lovastatin (5mg/kg ; 14 days ; Intraperitoneal injection) attenuates hippocampal cell death in Pilocarpine-induced status epilepticus rat model through downregulation of the pro-apoptotic Mst1 gene[6]. Lovastatin (0.5mg/kg ; 10 days ; subcutaneous injection) enhanced ovarian activity throughout follicular development in ICR mice model[7].
Scheme of Low-Density Lipoprotein Receptor（LDLR）activity signaling pathway for follicular development with lovastatin stimulates steroidogenesis in ovaries[7].
References:
[1] AMADASU E, KANG R, USMANI A, et al. Effects of Lovastatin on Brain Cancer Cells [J]. Cell Transplant, 2022, 31(9636897221102903.
[2] H BISCHOFF R A, M BOBERG, D PETZINNA, D SCHMIDT, W STEINKE, G THOMAS. Preclinical review of cerivastatin sodium--a step forward in HMG-CoA reductase inhibition [J]. 1998,
[3] BORUTA T, BIZUKOJC M. Production of lovastatin and itaconic acid by Aspergillus terreus: a comparative perspective [J]. World J Microbiol Biotechnol, 2017, 33(2): 34.
[4] CEREZO-GUISADO M I, GARCIA-ROMAN N, GARCIA-MARIN L J, et al. Lovastatin inhibits the extracellular-signal-regulated kinase pathway in immortalized rat brain neuroblasts [J]. Biochem J, 2007, 401(1): 175-83.
[5] LIU S, YANG P, WANG M, et al. Inhibitory effect of lovastatin on human lung cancer cell proliferation by regulating the ERK1/2 and COX-2 pathways [J]. Transl Cancer Res, 2022, 11(4): 813-22.
[6] ABDANIPOUR A, DEHESHJO F, SOHRABI D, et al. Neuroprotective effect of lovastatin through down-regulation of pro-apoptotic Mst1 gene expression in rat model pilocarpine epilepsy [J]. Neurol Res, 2018, 40(10): 874-82.
[7] KIM Y J, CHO Y I, JANG J, et al. Lovastatin, an Up-Regulator of Low-Density Lipoprotein Receptor, Enhances Follicular Development in Mouse Ovaries [J]. Int J Mol Sci, 2023, 24(8).
Lovastatin是一种3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，通过影响甲羟戊酸途径来发挥作用[1]，IC50值为77nM[2]。Lovastatin能抑制胆固醇合成[3]，EC50值为0.002mg/kg[2]。
Lovastatin能够在特定条件下诱导细胞凋亡，特别是在自发永生化的鼠脑神经母细胞中（10μM , 24小时）[4]。Lovastatin有效地抑制了Ras的激活，这与ERK1/2（细胞外信号调节激酶1/2）磷酸化的显著减少有关[4]。Lovastatin可以通过调节ERK1/2和COX-2信号通路来抑制A549（人肺腺癌细胞）的增殖（50μM , 24小时）[5]。
Lovastatin能通过下调促凋亡基因Mst1来减轻由Pilocarpine诱导的癫痫持续状态大鼠模型中海马的细胞死亡[6]。Lovastatin(0.5 mg/kg ；10天 ；皮下注射)增强了ICR小鼠在卵泡发育过程中的卵巢活性[7]。
通过激活低密度脂蛋白受体（LDLR）活性信号通路促进卵泡发育，并刺激卵巢中类固醇的生成方案[7]。
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Cell experiment[1]: |
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Cell lines |
Human Pancreatic ductal adenocarcinoma (PDAC) lines： MIA-PaCa-2 (MIA) . |
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Preparation method |
The cells were cultured in Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal bovine serum at 37℃ in 5% CO2 . The cells were treated with 0.5μM Lovastatine within 48h . |
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Reaction Conditions |
0.5μM within 48h . |
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Applications |
Lovastatin increased mitochondrial oxidative stress in PDAC cells , leading to apoptosis. |
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Animal experiment[2]: |
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Animal models |
Male Wistar rats . |
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Preparation method |
Rat model epilepsy was induced by an intraperitoneal injection of pilocarpine (350-400mg/kg for 30min) . All injections of Lovastatin were administered intraperitoneally in a final 0.5ml volume, 3 days following the first seizure on a daily basis for 14 days . |
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Dosage form |
5mg/kg ; 14 days ; Intraperitoneal injection. |
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Applications |
Lovastatin attenuates hippocampalcell death in Pilocarpine-induced status epilepticus rat model through downregulation of the pro-apoptotic Mst1 gene. |
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References: [1] GYOTEN M, LUO Y, FUJIWARA-TANI R, et al. Lovastatin Treatment Inducing Apoptosis in Human Pancreatic Cancer Cells by Inhibiting Cholesterol Rafts in Plasma Membrane and Mitochondria [J]. Int J Mol Sci, 2023, 24(23): [2] ABDANIPOUR A, DEHESHJO F, SOHRABI D, et al. Neuroprotective effect of lovastatin through down-regulation of pro-apoptotic Mst1 gene expression in rat model pilocarpine epilepsy [J]. Neurol Res, 2018, 40(10): 874-82. |
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| 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 | |||
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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 |
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| 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 |
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| % 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，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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