| E6038 |
Pitavastatin
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Pitavastatin (NK-104) is a highly potent inhibitor of HMG-CoA Reductase with an IC50 of 6.8 nmol/L, which significantly enhances LDL receptor activity and lowers LDL cholesterol (LDL-C) levels. It also inhibits cholesterol synthesis in vitro and has the potential to manage hypercholesterolemia and reducing cardiovascular risk.
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Nat Commun, 2025, 16(1):5360
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Biochem Biophys Res Commun, 2025, 742:151094
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JCI Insight, 2024, 9(24)e178535
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| S8302 |
SR-12813
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SR-12813 is a pregnane X receptor (PXR) agonist and HMG-CoA reductase inhibitor with an IC50 of 850 nM.
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Front Pharmacol, 2024, 15:1488367
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Evid Based Complement Alternat Med, 2021, 2021:4358163
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Cell Death Dis, 2019, 10(10):777
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| S2664 |
Clinofibrate
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Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood.
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Carcinogenesis, 2020, 7;bgaa036
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| E4981 |
Fluvastatin
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Fluvastatin is a competitive inhibitor of HMG-CoA reductase with an IC50 value of 40 and 100 nM in human liver microsomes. This compound also exerts cytoprotective effects against oxidative stress through the Nrf2-dependent antioxidant pathway.
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JCI Insight, 2024, 9(24)e178535
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| E4821 |
Simvastatin acid (ammonium)
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Simvastatin acid (Tenivastatin) ammonium is a potent inhibitor of HMG-CoA reductase (HMGCR). This compound also decreases Indoxyl sulfate-induced reactive oxygen species (ROS) production in human cardiomyocytes and regulates the expression of OATP3A1 in these cells.
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| E1341 |
Cerivastatin sodium
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Cerivastatin sodium, a sodium salt of cerivastatin, is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase with Ki of 1.3 nM. It is also a synthetic, enantiomerically pure, pyridine derivative that effectively reduces serum cholesterol levels at microgram doses.
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| E4792 |
Atorvastatin calcium hydrate
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Atorvastatin calcium hydrate (Totalip) is a potent inhibitor of the HMG-CoA Reductase. It is used as a potent hypolipidemic agent to reduce the elevated total-cholesterol, low-density lipoprotein (LDL), apolipoprotein B (apo B), and triglyceride (TG) levels, and to increase the high-density lipoprotein cholesterol (HDL-C) level in patients with primary hypercholesterolemia and mixed dyslipidemia.
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| E2286 |
Dihydrolanosterol
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Dihydrolanosterol (24,25-Dihydrolanosterol; Dihydrolanosterin; Lanostenol) inhibits cholesterol biosynthesis by promoting ubiquitination and degradation of HMG-CoA Reductase.
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| E2741 |
7-ketocholesterol
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7-Ketocholesterol (7-Oxocholesterol), is a bioactive sterol and prominent cholesterol oxidation product, is a strong inhibitor of HMG-CoA Reductase and cytochrome P450 7A1. It enhances oxidative stress, endoplasmic reticulum stress, and apoptosis in macrophages.
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