Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H37O6.Na |
| Molecular Weight | 444.5367 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 8 / 8 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[H][C@]12[C@H](C[C@@H](C)C=C1C=C[C@H](C)[C@@H]2CC[C@@H](O)C[C@@H](O)CC([O-])=O)OC(=O)[C@@H](C)CC
InChI
InChIKey=LXZBFUBRYYVRQJ-AXHZAXLDSA-M
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
| Molecular Formula | C24H37O6 |
| Molecular Weight | 421.547 |
| Charge | -1 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 8 / 8 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | Na |
| Molecular Weight | 22.9898 |
| Charge | 1 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019643s085lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021316s031lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20467214
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019643s085lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021316s031lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20467214
Lovastatin is a cholesterol-lowering agent that belongs to the class of medications called statins. Alfred Alberts and his team at Merck discovered it in 1978 after screening only 18 compounds over 2 weeks. The agent, also known as mevinolin, was isolated from the fungi Aspergillus terreus. Research on this compound was suddenly shut down in 1980 and the drug was not approved until 1987. Interesting, Akira Endo at Sankyo Co. (Japan) patented lovastatin isolated from Monascus ruber four months before Merck. Lovastatin was found to be 2 times more potent than its predecessor, mevastatin, the first discovered statin. The primary uses of lovastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. Lovastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, a strong inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate. The conversion of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol. Lovastatin, as well as some of its metabolites, are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. The involvement of low-density lipoprotein cholesterol (LDL-C) in atherogenesis has been well documented in clinical and pathological studies, as well as in many animal experiments. Epidemiological and clinical studies have established that high LDL-C and low high-density lipoprotein cholesterol (HDL-C) levels are both associated with coronary heart disease. However, the risk of developing coronary heart disease is continuous and graded over the range of cholesterol levels and many coronary events do occur in patients with total cholesterol (Total-C) and LDL-C levels in the lower end of this range. Lovastatin immediate-release tablets have been shown to reduce elevated LDL-C concentrations. LDL is formed from very low-density lipoprotein (VLDL) and is catabolized predominantly by the high-affinity LDL receptor. The mechanism of the LDL-lowering effect of lovastatin immediate-release may involve both reduction of VLDL-C concentration, and induction of the LDL receptor, leading to reduced production and/or increased catabolism of LDL-C.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL402 |
0.64 nM [IC50] | ||
Target ID: CHEMBL402 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | ALTOPREV Approved Use1.1 Prevention of Coronary Heart Disease In patients without symptomatic coronary heart disease (CHD), but at high risk, Altoprev® is indicated to reduce the risk of: Myocardial infarction; Unstable angina; Coronary revascularization procedures; Coronary Heart Disease. Altoprev is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower Total-C and LDL-C to target levels. Hyperlipidemia Altoprev is indicated as an adjunct to diet for the reduction of elevated Total-C, LDL-C, Apo B, and TG, and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb). Launch Date1.01200318E12 |
|||
| Palliative | ALTOPREV Approved Use1.1 Prevention of Coronary Heart Disease In patients without symptomatic coronary heart disease (CHD), but at high risk, Altoprev® is indicated to reduce the risk of: Myocardial infarction; Unstable angina; Coronary revascularization procedures; Coronary Heart Disease. Altoprev is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower Total-C and LDL-C to target levels. Hyperlipidemia Altoprev is indicated as an adjunct to diet for the reduction of elevated Total-C, LDL-C, Apo B, and TG, and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb). Launch Date1.01200318E12 |
|||
| Preventing | MEVACOR Approved UseAfter oral ingestion, lovastatin, which is an inactive lactone, is hydrolyzed to the lovastatin acid. This is a principal metabolite and an inhibitor of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, which is an early and rate limiting step in the biosynthesis of cholesterol. Lovastatin has been shown to reduce both normal and elevated low-density lipoprotein cholesterol (LDL-C). Launch Date5.5728E11 |
|||
| Primary | MEVACOR Approved UseTherapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. MEVACOR is indicated as an adjunct to diet for the reduction of elevated total-C and LDL-C levels in patients with primary hypercholesterolemia (Types IIa and IIb***), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate. Launch Date5.5728E11 |
|||
| Secondary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
17.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
11.9 ng/mL |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
76.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
83 ng × h/mL |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5% |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Disc. AE: Aspartate aminotransferase increased, Alanine aminotransferase increased... AEs leading to discontinuation/dose reduction: Aspartate aminotransferase increased (grade 2-4, 1.3%) Sources: Page: p.1082, 1083Alanine aminotransferase increased (grade 2-4, 1.3%) Gastrointestinal disturbance (0.4%) Rash (0.27%) Myalgia (0.13%) Myopathy (0.27%) Arthralgia (0.13%) Insomnia (0.13%) Weight gain (0.13%) |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
DLT: Creatine phosphokinase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Creatine phosphokinase increased (grade 4, 33.3%) Sources: Page: p.527Aspartate aminotransferase increased (grade 2-3, 33.3%) Alanine aminotransferase increased (grade 2-3, 33.3%) |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
DLT: Creatine phosphokinase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Creatine phosphokinase increased (grade 4, 28.6%) Sources: Page: p.527Aspartate aminotransferase increased (grade 3, 14.3%) Alanine aminotransferase increased (grade 3, 14.3%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Arthralgia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Insomnia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Myalgia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Weight gain | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Myopathy | 0.27% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Rash | 0.27% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Gastrointestinal disturbance | 0.4% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Alanine aminotransferase increased | grade 2-4, 1.3% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Aspartate aminotransferase increased | grade 2-4, 1.3% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
| Alanine aminotransferase increased | grade 2-3, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
| Aspartate aminotransferase increased | grade 2-3, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
| Creatine phosphokinase increased | grade 4, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
| Alanine aminotransferase increased | grade 3, 14.3% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
| Aspartate aminotransferase increased | grade 3, 14.3% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
| Creatine phosphokinase increased | grade 4, 28.6% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery, biochemistry and biology of lovastatin. | 1988 Nov 11 |
|
| Coronary angiographic changes with lovastatin therapy. The Monitored Atherosclerosis Regression Study (MARS). | 1993 Nov 15 |
|
| Two different types of exercise-induced muscle pain without myopathy and CK-elevation during HMG-Co-enzyme-A-reductase inhibitor treatment. | 1999 Apr |
|
| Statins and peripheral neuropathy. | 1999 Jan |
|
| Effect of lipid-lowering strategies on tubular cell biology. | 1999 Jul |
|
| Lovastatin-induced apoptosis of human medulloblastoma cell lines in vitro. | 1999 Mar |
|
| The cyclin dependent kinase inhibitor p27 and its prognostic role in breast cancer. | 2001 |
|
| Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. | 2001 Apr |
|
| A new simvastatin (mevinolin)-resistance marker from Haloarcula hispanica and a new Haloferax volcanii strain cured of plasmid pHV2. | 2001 Apr |
|
| Comparative study of HMG-CoA reductase inhibitors on fibrinogen. | 2001 Apr |
|
| Cell cycle-related changes in regulatory volume decrease and volume-sensitive chloride conductance in mouse fibroblasts. | 2001 Apr |
|
| The biosynthetic incorporation of the intact leucine skeleton into sterol by the trypanosomatid Leishmania mexicana. | 2001 Apr 13 |
|
| Statins are magic when you gotta have heart. | 2001 Apr 16 |
|
| Assessing the results: phase 1 hyperlipidemia outcomes in 27 health plans. | 2001 Apr 16 |
|
| Deterioration of the protein kinase C-K(ATP) channel pathway in regulation of coronary flow in hypercholesterolaemic rabbits. | 2001 Apr 27 |
|
| Interaction of cytosine arabinoside and lovastatin in human leukemia cells. | 2001 Aug |
|
| [Statins: intervention studies, facts and perspectives]. | 2001 Feb |
|
| [Statins and diabetic hyperlipidemia]. | 2001 Feb |
|
| [Statins and stroke]. | 2001 Feb |
|
| [Mechanisms of action of statins and their pleiotropic effects]. | 2001 Feb |
|
| Do HMG-CoA reductase inhibitors affect fibrinogen? | 2001 Feb |
|
| Bimonthly update. Therapy and clinical trials. | 2001 Feb |
|
| Nitrogen-bisphosphonates block retinoblastoma phosphorylation and cell growth by inhibiting the cholesterol biosynthetic pathway in a keratinocyte model for esophageal irritation. | 2001 Feb |
|
| Butyrate-induced differentiation of Caco-2 cells occurs independently from p27. | 2001 Feb 23 |
|
| Rhabdomyolysis secondary to a drug interaction between simvastatin and clarithromycin. | 2001 Jan |
|
| Fragmentation study of simvastatin and lovastatin using electrospray ionization tandem mass spectrometry. | 2001 Jan |
|
| Statins in children: what do we know and what do we need to do? | 2001 Jan |
|
| Effective use of statins to prevent coronary heart disease. | 2001 Jan 15 |
|
| [The role of HDL in the prevention of cardiovascular events]. | 2001 Jan 21 |
|
| Low-dose combination therapy with colesevelam hydrochloride and lovastatin effectively decreases low-density lipoprotein cholesterol in patients with primary hypercholesterolemia. | 2001 Jun |
|
| Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. | 2001 Jun |
|
| HMG-CoA reductase inhibitors and P-glycoprotein modulation. | 2001 Mar |
|
| A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. | 2001 Mar |
|
| 3-Hydroxy-3-methylglutaryl coenzyme A synthase-1 of Blattella germanica has structural and functional features of an active retrogene. | 2001 Mar 15 |
|
| Liver regeneration after hepatectomy. | 2001 Mar-Apr |
|
| New OTC drugs and devices 2000: a selective review. | 2001 Mar-Apr |
|
| The National Service Framework on coronary heart disease: is it sufficiently evidence-based? | 2001 May |
|
| Statin induced myopathy does not show up in MIBI scintigraphy. | 2001 May |
|
| Can modulation of endothelial nitric oxide synthase explain the vasculoprotective actions of statins? | 2001 May |
|
| Cholesterol ester accumulation: an immediate consequence of acute in vivo ischemic renal injury. | 2001 May |
|
| Air Force/Texas Coronary Atherosclerosis Prevention Study (AFCAPS/TEXCAPS): additional perspectives on tolerability of long-term treatment with lovastatin. | 2001 May 1 |
|
| Cost effectiveness of HMG-CoA reductase inhibition in Canada. | 2001 Spring |
Patents
Sample Use Guides
Lovastatin is administered orally with the evening meal. Maximal daily dose for adults is 80 mg, maximal dose for children is 40 mg.
Route of Administration:
Oral
HMG-CoA reductase from rat liver microsomes was solubilizes and purified through the second ammonium sulfate precipitation. Prior to use, the enzyme was activated at 37C for 30 min. The reaction mix contained, in 100 uL: 0.14 M potassium phosphate buffer, pH 6.8; 0.18 M KCI; 3.5 mM EDTA, pH 7.0; 10 mM dithiothreitol; bovine serum albumin at 0.1 mg/ml; 0.02 uCi of [14C]HMG-CoA and 0.3 pg of partially purified enzyme (specific activity 100-150 nmol min-1 mg-1) with or without inhibitor. After 5-min incubation at 37C, the reaction was initiated with 0.2 mM NADPH. The reaction was terminated with 20 Al of 5 M HCL. After an additional incubation for 15 min at 370C to allow for complete lactonization of the product, mevalonate, the mixture was passed over a 0.5 X 5 cm column containing 100-200 mesh Bio-Rex, chloride form (Bio-Rad), which was equilibrated with distilled water. With this resin the unreacted [14C]HMG-CoA was adsorbed and the product, [14C]mevalonolactone, was eluted with 3 ml of distilled water directly into scintillation vials. After the addition of 10 ml of Aquasol II, radioactivities of the samples were measured in a scintillation counter. Lovastatin acid inhibited HMG-CoA reductase with Ki of 0.64 nM.
| Substance Class |
Chemical
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LK08RY63S3
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PARENT -> SALT/SOLVATE |
