Lovastatin (Synonyms: (+)-Mevinolin, Monacolin K, NSC 633781) |
| Catalog No.GC11633 |
Lovastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that impacts the mevalonate pathway, which has an IC50 value of 77nM.
Products are for research use only. Not for human use. We do not sell to patients.
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).
|
Cell experiment[1]: |
|
|
Cell lines |
Human Pancreatic ductal adenocarcinoma (PDAC) lines： MIA-PaCa-2 (MIA) . |
|
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 . |
|
Reaction Conditions |
0.5μM within 48h . |
|
Applications |
Lovastatin increased mitochondrial oxidative stress in PDAC cells , leading to apoptosis. |
|
Animal experiment[2]: |
|
|
Animal models |
Male Wistar rats . |
|
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 . |
|
Dosage form |
5mg/kg ; 14 days ; Intraperitoneal injection. |
|
Applications |
Lovastatin attenuates hippocampalcell death in Pilocarpine-induced status epilepticus rat model through downregulation of the pro-apoptotic Mst1 gene. |
|
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. |
|
| Cas No. | 75330-75-5 | SDF | |
| Synonyms | (+)-Mevinolin, Monacolin K, NSC 633781 | ||
| Chemical Name | [(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 | ||
| Formula | C24H36O5 | M.Wt | 404.54 |
| Solubility | ≥ 20.2 mg/mL in DMSO, ≥ 18.6 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *