| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Lovastatin Sodium targets HMG-CoA reductase (HMGCR), the rate-limiting enzyme in the cholesterol biosynthesis pathway. It acts as a competitive inhibitor of the enzyme, blocking the conversion of HMG-CoA to mevalonate. By inhibiting this enzyme, it decreases cholesterol production and increases LDL receptor-mediated uptake of LDL cholesterol from the bloodstream.
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|---|---|
| ln Vitro |
Mevalonate: NADP+ oxidoreductase (CoA acylation)] is a strong competitive inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase. Mevinolin's hydroxy acid form, mevinolinic Acid, is one such inhibitor[1].
In vitro, lovastatin sodium inhibits cholesterol and isoprenoid biosynthesis by inhibiting HMG-CoA reductase (Ki for the acid form is 1 nM). It blocks protein isoprenylation. It is active in whole cells as well as cell-free assays. Specific IC₅₀ values vary by assay and cell type. |
| ln Vivo |
In vivo, lovastatin sodium reduces plasma cholesterol levels in humans. It is the active form of lovastatin, used to treat hypercholesterolemia. It has been shown to effectively lower LDL cholesterol and total cholesterol in clinical studies. The sodium salt form is used in research applications.
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| Enzyme Assay |
HMG-CoA reductase enzyme activity is measured using cell-free assays with purified enzyme or microsomal preparations. The assay involves incubation with [¹⁴C]-HMG-CoA and NADPH. Product formation (mevalonate) is quantified by scintillation counting after separation. Lovastatin sodium is tested at various concentrations, and Ki values are calculated.
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| Cell Assay |
Cultured cells (e.g., HepG2, fibroblasts) are treated with lovastatin sodium at various concentrations for 24-72 hours. Cholesterol synthesis is assessed by measuring [¹⁴C]-acetate incorporation into sterols. LDL receptor expression is measured by Western blot or flow cytometry. Cell viability and cytotoxicity are assessed by MTT assay.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of hypercholesterolemia (e.g., high-fat diet-fed rodents, Watanabe heritable hyperlipidemic rabbits). Lovastatin sodium is administered orally or intraperitoneally. Serum lipid profiles (total cholesterol, LDL, HDL, triglycerides) are measured. Liver HMG-CoA reductase activity and LDL receptor expression are assessed.
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| ADME/Pharmacokinetics |
Lovastatin Sodium is the active hydroxy acid form of lovastatin. It is well-absorbed orally and undergoes extensive first-pass metabolism. It is metabolized in the liver primarily by CYP3A4. It has a short half-life (~1-2 hours) and is excreted primarily in feces. It is highly protein-bound. The sodium salt form is used in research applications.
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| Toxicity/Toxicokinetics |
Lovastatin Sodium shares the toxicity profile of lovastatin. Common adverse effects include myalgia, elevated liver enzymes, and gastrointestinal disturbances. Rare but serious adverse effects include rhabdomyolysis and hepatotoxicity. It is contraindicated during pregnancy and in patients with active liver disease. Drug interactions occur with CYP3A4 inhibitors.
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| References | |
| Additional Infomation |
Lovastatin Sodium (Mevinolinic acid sodium) is the pharmacologically active open-ring hydroxy acid form of lovastatin. It is used in research to study HMG-CoA reductase inhibition and cholesterol metabolism. It is not the clinically administered form (lovastatin is administered as a lactone prodrug) but is the active species responsible for the pharmacological effects of lovastatin therapy.
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| Molecular Formula |
C24H37NAO6
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|---|---|
| Molecular Weight |
444.54
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| Exact Mass |
444.248
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| CAS # |
75225-50-2
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| Related CAS # |
Lovastatin acid;75225-51-3;Lovastatin-d3 hydroxy acid sodium;1217528-38-5
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| PubChem CID |
16760544
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
602.3ºC at 760 mmHg
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| Melting Point |
154-160ºC
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| Flash Point |
199.1ºC
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| LogP |
2.38
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
31
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| Complexity |
661
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC[C@H](C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@H](C[C@H](CC(=O)[O-])O)O)C.[Na+]
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| InChi Key |
LXZBFUBRYYVRQJ-AXHZAXLDSA-M
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| InChi Code |
InChI=1S/C24H38O6.Na/c1-5-15(3)24(29)30-21-11-14(2)10-17-7-6-16(4)20(23(17)21)9-8-18(25)12-19(26)13-22(27)28;/h6-7,10,14-16,18-21,23,25-26H,5,8-9,11-13H2,1-4H3,(H,27,28);/q;+1/p-1/t14-,15-,16-,18+,19+,20-,21-,23-;/m0./s1
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| Chemical Name |
sodium;(3R,5R)-7-[(1S,2S,6R,8S,8aR)-2,6-dimethyl-8-[(2S)-2-methylbutanoyl]oxy-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoate
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| Synonyms |
Mevinolin sodium Lovastatin Na Lovastatin Sodium
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~12.5 mg/mL (~28.12 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2495 mL | 11.2476 mL | 22.4952 mL | |
| 5 mM | 0.4499 mL | 2.2495 mL | 4.4990 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2495 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.
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