[CAS NO. 75330-75-5] Lovastatin

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PRODUCTS SPECIFICATIONS [75330-75-5]

Catalog

HY-N0504

Brand

MCE

CAS

75330-75-5

DESCRIPTION [75330-75-5]

Overview

MDL	MFCD00072164
Molecular Weight	404.54
Molecular Formula	C24H36O5
SMILES	O=C([C@@H](C)CC)O[C@@H]1[C@@]([C@H]2CC[C@@H](OC3=O)C[C@H](C3)O)([H])C(C=C[C@@H]2C)=C[C@H](C)C1

For research use only. We do not sell to patients.

14 Publications Citing Use of MCE

Summary

Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol .

IC50 & Target

HMG-CoA reductase ^[1]

In Vitro

Lovastatin (10 μM; 72 hours) efficiently reduces viability of HepG2 cells ^[2] .
Lovastatin (10 μM; 48 hours) induces apoptosis in HepG2 cells ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[2]

Cell Line:	HepG2 cells
Concentration:	10 μM
Incubation Time:	72 hours
Result:	Efficiently reduced viability of HepG2 cells.

In Vivo

Lovastatin is an inactive lactone that is hydrolyzed in the liver to an active f3-hydroxyacid form. This principal metabolite is the inhibitor of the enzyme HMG-CoA reductase. The K _i is 1 nM. Lovastatin and its β-hydroxyacid metabolite are highly bound to human plasma proteins. Lovastatin crosses the blood-brain and placental barriers ^[3] . Lovastatin produces a profound reduction of apolipoprotein-B-containing lipoproteins, especially LDL cholesterol and, to a lesser extent, plasma triglycerides, and a small increase in HDL cholesterol ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03510715	Sanofi\|Regeneron Pharmaceuticals	Hypercholesterolemia	August 31, 2018	Phase 3
NCT01250535	University of North Carolina, Chapel Hill\|National Institutes of Health (NIH)	Healthy Volunteers\|Drug Drug Interactions	December 2010	Phase 1
NCT00583102	University of Iowa	Acute Myeloid Leukemia	June 2001	Phase 1\|Phase 2
NCT00132717	Organon and Co	Hypercholesterolemia	January 1, 2005	Phase 3
NCT02518503	Canadian Network for Observational Drug Effect Studies, CNODES\|Drug Safety and Effectiveness Network, Canada\|Canadian Institutes of Health Research (CIHR)	Diabetes Mellitus, Type 2\|Cardiovascular Disease	July 2012
NCT00741013	Washington University School of Medicine\|Barnes-Jewish Hospital	Lung Inflammation	March 2007	Early Phase 1
NCT00000512	University of Washington\|National Heart, Lung, and Blood Institute (NHLBI)	Cardiovascular Diseases\|Coronary Arteriosclerosis\|Coronary Disease\|Heart Diseases\|Myocardial Ischemia	January 1984	Phase 3
NCT04297033	Beijing Tiantan Hospital	Cerebral Arteriovenous Malformation	January 1, 2021	Phase 2
NCT00243880	Columbia University	Stroke	September 2005	Phase 1
NCT03981601	Islamic Azad University, Tehran	Bone Loss	February 22, 2018	Phase 2
NCT00352599	University of California, Los Angeles	Neurofibromatosis 1	September 2009	Phase 1
NCT01976936	Mitchell S Elkind\|National Institute of Neurological Disorders and Stroke (NINDS)\|Columbia University	Stroke\|Rhabdomyolysis\|Jaundice	February 2009	Phase 2
NCT00585052	University of Iowa	Ovarian Cancer	August 2003	Phase 2
NCT00584012	Susan L Roeder\|University of Iowa	Any Cancer\|Breast Cancer	April 2004	Phase 1
NCT00092846	Merck Sharp & Dohme LLC	Hypercholesterolemia	December 4, 2002	Phase 3
NCT00685685	Mutual Pharmaceutical Company, Inc.	Healthy	September 2004	Phase 1
NCT02603770	Luye Pharma Group Ltd.	Lipid Metabolism Disorder	November 2015	Phase 1
NCT00004346	National Center for Research Resources (NCRR)\|Oregon Health and Science University	Cerebrotendinous Xanthomatosis	January 1996	Phase 2
NCT00700921	National Jewish Health\|National Heart, Lung, and Blood Institute (NHLBI)	Chronic Obstructive Pulmonary Disease (COPD)	April 2008	Phase 2
NCT03178526	Islamic Azad University, Tehran	Alveolar Bone Loss, Chronic Periodontitis, Lovestatin Gel, Regeneration	December 24, 2015	Phase 2\|Phase 3
NCT00000463	National Heart, Lung, and Blood Institute (NHLBI)	Cardiovascular Diseases\|Coronary Disease\|Heart Diseases\|Myocardial Ischemia	April 1987	Phase 3
NCT00000469	National Heart, Lung, and Blood Institute (NHLBI)	Cardiovascular Diseases\|Carotid Stenosis\|Cerebral Arteriosclerosis\|Cerebrovascular Disorders\|Heart Diseases\|Vascular Diseases	May 1988	Phase 2
NCT02518516	Canadian Network for Observational Drug Effect Studies, CNODES\|Drug Safety and Effectiveness Network, Canada\|Canadian Institutes of Health Research (CIHR)	Hypercholesterolemia	January 2011
NCT03242499	National Taiwan University Hospital	Parkinson Disease	May 15, 2017	Phase 2
NCT00116870	Merck Sharp & Dohme LLC\|National Institute on Aging (NIA)	Atherosclerosis\|Coronary Artery Disease	June 1985	Phase 2\|Phase 3
NCT00580970	Virginia Commonwealth University\|Hunter Holmes Mcguire Veteran Affairs Medical Center	Prostate Cancer	April 2007	Phase 2
NCT00721305	Universidad de Antioquia\|Instituto Colombiano para el Desarrollo de la Ciencia y la Tecnología (COLCIENCIAS)\|Laboratorio Clínico Congregación Mariana\|Laboratorios Laproff S.A.\|Humax Pharmaceutical	HIV Seropositivity	August 2008	Phase 2
NCT02563860	Montefiore Medical Center\|Rett Syndrome Research Trust	Rett Syndrome	July 2015	Phase 2
NCT01478828	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Patrick C Walsh Prostate Cancer Research Fund	Prostate Cancer	July 13, 2012	Not Applicable
NCT00071266	Kos Pharmaceuticals	Intermittent Claudication\|Peripheral Vascular Disease	October 2003	Phase 3
NCT00302952	National Institute of Allergy and Infectious Diseases (NIAID)\|Autoimmunity Centers of Excellence	Rheumatoid Arthritis	November 6, 2007	Phase 2
NCT00963664	NeoPlas Innovation	Melanoma\|Malignant Melanoma	December 2009	Phase 2
NCT02642653	University of California, Davis	Fragile X Syndrome\|Genetic Diseases	January 2016	Phase 4
NCT03826940	University of Coimbra	Autism Spectrum Disorder\|Neurofibromatosis 1	February 19, 2019	Not Applicable
NCT01110642	Northwestern University	Syndromic Ichthyoses\|CHILD Syndrome\|Smith Lemli Opitz Syndrome\|Conradi Syndrome	July 2011	Phase 2
NCT04359823	Medical University of South Carolina	Actinic Porokeratosis	August 24, 2020	Phase 1\|Phase 2
NCT03510884	Sanofi\|Regeneron Pharmaceuticals	Hypercholesterolaemia	May 31, 2018	Phase 3
NCT00689806	University of Chicago	Severe Persistent Asthma		Phase 1\|Phase 2
NCT00902668	Virginia Commonwealth University	Breast Cancer\|Radiation Toxicity	April 2009	Phase 2
NCT01527669	National Taiwan University Hospital\|National Science Council, Taiwan	Healthy Subjects	February 2012	Phase 4
NCT02998151	Children´s Hospital Medical Center, Cincinnati\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	Fragile X Syndrome	January 2016	Early Phase 1
NCT02964884	Vanderbilt University\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	Neurofibromatosis Type 1\|Learning Disability\|Reading Disability\|NF1	November 2016	Phase 2
NCT00000477	National Heart, Lung, and Blood Institute (NHLBI)	Atherosclerosis\|Cardiovascular Diseases\|Coronary Disease\|Heart Diseases\|Hypercholesterolemia\|Myocardial Ischemia	July 1990	Phase 2
NCT02389868	Université de Sherbrooke	Blood Platelets Proteome	February 2015	Phase 2
NCT00285857	Stanford University	Breast Cancer	November 2005	Phase 2
NCT00462280	National Cancer Institute (NCI)	Precancerous Condition\|Stage 0 Melanoma\|Stage I Melanoma\|Stage II Melanoma	May 2007	Phase 2
NCT00853580	University of Alabama at Birmingham\|Boston Children´s Hospital\|Children´s Hospital of Philadelphia\|Children´s National Research Institute\|Children´s Hospital Medical Center, Cincinnati\|National Cancer Institute (NCI)\|University of Chicago\|University of Utah\|Washington University School of Medicine\|Sydney Children´s Hospitals Network\|University of Texas Southwestern Medical Center	Neurofibromatosis Type 1	July 2009	Phase 2
NCT00062556	Kos Pharmaceuticals	Intermittent Claudication\|Peripheral Vascular Disease	January 2003	Phase 3
NCT03504501	Technical University of Munich	Impaired Synaptic Plasticity\|Impaired Cognition	March 22, 2019	Phase 2
NCT00684723	Mutual Pharmaceutical Company, Inc.	Healthy	July 2004	Phase 1

Appearance

Solid

Source

aspergillus terreus

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 247.19 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Butanoic acid, 2-methyl-, (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester, (2S)-

Butanoic acid, 2-methyl-, 1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester, [1S-[1α(R*),3α,7β,8β(2S*,4S*),8aβ]]-

Mevinolin

MSD 803

Monacolin K

Antibiotic MB 530B

MK 803

Monacolin K lactone

Lovastatin

Mevacor

L 154803

(+)-Mevinolin

6α-Methylcompactin

Sivlor

Mevlor

Lovalip

Mevinacor

Altocor

Lovastatin lactone

Lostatin

Lestric

Lovacard

Lovex

Altoprev

NSC 633781