Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Lovastatin (Mevinolin; Mevacor; MK-803; Altoprev; Monacolin K; MK803), belonging to the statin class of hypolipidemic agent/lipid-lowering drugs, is a potent and cell-permeable inhibitor of HMG-CoA reductase with potential anti-hyperlipidemic effects. It inhibits HMG-CoA reductase with an IC50 of 3.4 nM in a cell-free assay. Lovastatin has been approved for use in reducing/lowering cholesterol.
ln Vitro |
HepG2 cell viability is effectively reduced by lovastatin (10 μM; 72 hours)[2]. In HepG2 cells, lovastatin (10 μM; 48 hours) causes apoptosis [2].
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ln Vivo |
The liver hydrolyzes the inactive lactone lovastatin to produce the active f3-hydroxy acid form. This primary metabolite inhibits the enzyme HMG-CoA reductase. Ki is one nanometer. Human plasma proteins bind lovastatin and its beta-hydroxy acid metabolite tightly. Both the placental and blood-brain barriers are crossed by lovastatin [3]. Lovastatin modestly raises HDL cholesterol while considerably lowering apolipoprotein B-containing lipoproteins, particularly LDL cholesterol, and plasma triglycerides to a lesser level [4].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: HepG2 cells Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Efficiently decreased viability of HepG2 cells. |
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Animal Protocol |
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References |
[1]. Alberts AW, et al. Discovery, biochemistry and biology of lovastatin. Am J Cardiol. 1988 Nov 11;62(15):10J-15J.
[2]. Kah J, et al. Selective induction of apoptosis by HMG-CoA reductase inhibitors in hepatoma cells and dependence on p53 expression. Oncol Rep. 2012 Sep;28(3):1077-83. [3]. Frishman WH, et al. Lovastatin: an HMG-CoA reductase inhibitor for lowering cholesterol. Med Clin North Am. 1989 Mar;73(2):437-48. [4]. 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. [5]. Ifergan I, et al. Statins reduce human blood-brain barrier permeability and restrict leukocyte migration: relevance to multiple sclerosis. Ann Neurol. 2006 Jul;60(1):45-55. |
Molecular Formula |
C24H36O5
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Molecular Weight |
404.54
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CAS # |
75330-75-5
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Related CAS # |
Lovastatin (Standard);75330-75-5;Lovastatin-d9;Lovastatin-d3;1002345-93-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O(C([C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)[C@@]1([H])C([H])([H])[C@@]([H])(C([H])([H])[H])C([H])=C2C([H])=C([H])[C@]([H])(C([H])([H])[H])[C@]([H])(C([H])([H])C([H])([H])[C@]3([H])C([H])([H])[C@]([H])(C([H])([H])C(=O)O3)O[H])[C@@]12[H]
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL |
Preparing Stock Solutions | 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 | 1.2360 mL | 2.4719 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04297033 | Not yet recruiting | Drug: Lovastatin Drug: Placebo |
Cerebral Arteriovenous Malformation | Beijing Tiantan Hospital | January 1, 2021 | Phase 2 |
NCT01527669 | Completed | Drug: LipoCol Forte capsules Drug: Lovastatin Tablet |
Healthy Subjects | National Taiwan University Hospital | February 2012 | Phase 4 |
NCT00585052 | Terminated Has Results | Drug: Paclitaxel Drug: Lovastatin |
Ovarian Cancer | University of Iowa | August 2003 | Phase 2 |
NCT01346670 | Completed | Drug: LipoCol and Mevacor | Healthy Volunteer | Taipei Medical University WanFang Hospital |
October 2006 | Phase 4 |
FLV, SMV and LOV dose-dependently and selectively reduce viability of mouse hepatoma cells. Primary mouse hepatocytes (PH) or mouse hepatoma cells (Hepa1-6) were incubated in the presence of fluvastatin (FLV; A), simvastatin (SMV; B), rosuvastatin (ROV; C), atorvastatin (ATV; D), or lovastatin (LOV; E) at 1, 10 or 100 μM for 72 h. Cell viability was measured by MTT assay. *P≤0.05 for statin vs. solvent incubated cells; #P≤0.05 for statin incubated PH vs. Hepa1-6 cells. (F) Primary human hepatocytes (PHhum) were incubated in the presence of FLV, SMV, ROV, ATV, or LOV at 10 μM for 72 h. Cell viability was measured by MTT assay. *P≤0.05 for statin vs. solvent incubated cells. td> |
FLV, SMV and LOV efficiently and selectively reduce viability of human hepatoma cell lines. (A) Human hepatoma cells (Huh7; HepG2) were incubated in the presence of fluvastatin (FLV), simvastatin (SMV), rosuvastatin (ROV), atorvastatin (ATV), or lovastatin (LOV) at 10 μM for 72 h. Cell viability was measured by MTT assay. *P≤0.05 for statin vs. solvent incubated cells. (B) Apoptosis induction was measured in Huh7 and HepG2 cells after 48 h statin incubation by caspase-3 activity assay. *P≤0.05 for statin vs. solvent incubated cells. (C) Proliferation of Huh7 and HepG2 cells was measured continuously over a period of 66 h using the impedance-based xCELLigence real-time cell analyzing system. Results are expressed as mean cell index normalized to the time-point of seeding to 96-well E-plates. (D Expression of proliferating cell nuclear antigen (PCNA) was measured in Huh7 and HepG2 human hepatoma cells by real-time RT-PCR. *P≤0.05. td> |
p53 expression of human hepatoma cell lines correlates to their susceptibility towards statins. (A) p53 protein expression was measured in human hepatoma cells (Huh7; HepG2) by Western blotting. (B) p53 protein expression was measured by Western blotting in Huh7 cells with stable knockdown of p53 (shp53) or Huh7 cells expressing control shRNA directed against E.coli polymerase (shneg). Huh7 shneg or Huh7 shp53 cells were incubated in the presence of 10 μM fluvastatin (FLV), simvastatin (SMV) or lovastatin (LOV) for 72 h. Cell viability was measured by MTT assay (C), apoptosis induction was measured by caspase-3 activity assay (D). Expression of proliferating cell nuclear antigen (PCNA) was measured by real-time RT-PCR. *P≤0.05 for Huh7 shneg vs. Huh7 shp53 cells. td> |