1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. HMG-CoA Reductase (HMGCR)

HMG-CoA Reductase (HMGCR)

HMG-CoA Reductase (HMGCR) is the rate-limiting enzyme for cholesterol synthesis in the conversion of HMG-CoA to mevalonate. HMGCR is found in eukaryotes and prokaryotes. The phylogenetic analysis has revealed two classes of HMG-CoA reductase, the Class I enzymes of eukaryotes and some archaea and the Class II enzymes of eubacteria and certain other archaea.

Both in eukaryotes and in archaebacteria the enzyme HMGCR is known to catalyze an early reaction unique to isoprenoid biosynthesis. In humans, the HMG-CoA reductase reaction is rate-limiting for the biosynthesis of cholesterol and therefore constitutes a prime target of drugs that reduce serum cholesterol levels.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0504S
    Epi lovastatin-d3
    Epi Lovastatin-d3 is the deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Epi lovastatin-d<sub>3</sub>
  • HY-119695S
    Simvastatin acid-d6
    Inhibitor
    Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
    Simvastatin acid-d<sub>6</sub>
  • HY-Z10518
    ((3R,5R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate) calcium(II)
    Control
    ((3R,5R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate) calcium(II) is an impurity found in bulk preparations of the HMG-CoA reductase inhibitor Rosuvastatin (HY-17504A).
    ((3R,5R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate) calcium(II)
  • HY-107265
    Lucidenic acid E
    Inhibitor
    Lucidenic acid E is a terpenoid from Ganoderma lucidum.
    Lucidenic acid E
  • HY-123672S
    Lovastatin-d3 hydroxy acid sodium
    Inhibitor
    Lovastatin-d3 hydroxy acid (sodium) is the deuterium labeled Lovastatin hydroxy acid sodium. Lovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM.
    Lovastatin-d<sub>3</sub> hydroxy acid sodium
  • HY-17504BR
    Rosuvastatin Sodium (Standard)
    Inhibitor
    Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin Sodium (Standard)
  • HY-117219
    SKF 104976
    Inhibitor
    SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin.
    SKF 104976
  • HY-B1189R
    Meglutol (Standard)
    Inhibitor
    Meglutol (Standard) is the analytical standard of Meglutol. This product is intended for research and analytical applications. Meglutol is a lipid-lowering agent. Meglutol can reduces cholesterol, triglycerides, serum β-lipoprotein, and phospholipids, and inhibits the activity of HMG-CoA reductase (a rate-limiting enzyme in cholesterol biosynthesis). Meglutol can induce significant lipid oxidative damage in brain tissue. It is promising for research in the field of cardiovascular diseases and metabolic diseases.
    Meglutol (Standard)
  • HY-B0589H
    Atorvastatin strontium
    Inhibitor
    Strontium atorvastatin is a cholesterol-lowering drug with activity in ameliorating cardiovascular disease-related events. Strontium atorvastatin exerts its biological activity by inhibiting HMG-CoA reductase in liver tissue. Strontium atorvastatin is also used to suppress dyslipidemia.
    Atorvastatin strontium
  • HY-B0144AR
    Pitavastatin (Standard)
    Inhibitor
    Pitavastatin (Standard) is the analytical standard of Pitavastatin. This product is intended for research and analytical applications. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
    Pitavastatin (Standard)
  • HY-169818
    Keto lovastatin
    Control
    Keto lovastatin is an impurity of Lovastatin (HY-N0504) with antibacterial activity. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Keto lovastatin
  • HY-106281R
    Bemfivastatin (Standard)
    Inhibitor
    Bemfivastatin (Standard) is the analytical standard of Bemfivastatin (HY-106281). This product is intended for research and analytical applications. Bemfivastatin (PPD 10558) is an orally active HMG-CoA Reductase (HMGCR) inhibitor. Bemfivastatin enhances the activity of liver extraction and reduces blood lipid levels. Bemfivastatin can be used for research of metabolic disease, such as hypercholesterolemia.
    Bemfivastatin (Standard)
  • HY-B0144R
    Pitavastatin Calcium (Standard)
    Inhibitor
    Pitavastatin (Calcium) (Standard) is the analytical standard of Pitavastatin (Calcium). This product is intended for research and analytical applications. Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
    Pitavastatin Calcium (Standard)
  • HY-14664R
    Fluvastatin (Standard)
    Inhibitor
    Fluvastatin (Standard) is the analytical standard of Fluvastatin. This product is intended for research and analytical applications. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
    Fluvastatin (Standard)
  • HY-108257R
    Atorvastatin sodium (Standard)
    Inhibitor
    Atorvastatin sodium (Standard) is the analytical standard of Atorvastatin (sodium) (HY-108257). This product is intended for research and analytical applications. Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin sodium (Standard)
  • HY-149310A
    Dim16 hydrochloride
    Inhibitor
    Dim16 hydrochloride is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC50 of 0.8 nM against human PCSK9 and an IC50 of 146.8 μM against HMG-CoAR. Dim16 hydrochloride disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 hydrochloride can be used in research related to hypercholesterolemia.
    Dim16 hydrochloride
  • HY-N0466R
    Rebaudioside A (Standard)
    Inhibitor
    Rebaudioside A (Standard) is the analytical standard of Rebaudioside A. This product is intended for research and analytical applications. Rebaudioside A is an orally effective steviol glycoside with high sweetness. Rebaudioside A acts as an inhibitor of α-glucosidase with an IC50 value of 35.01 μg/mL. Rebaudioside A increases the ATP/ADP ratio in β cells in a glucose-dependent manner, thereby inhibiting KATP channels, leading to membrane depolarization, calcium influx, and ultimately stimulating insulin secretion. Rebaudioside A activates the SREBP signaling pathway by inhibiting HMGCR, the rate-limiting enzyme in cholesterol synthesis, resulting in increased expression of LDLR on the cell surface, thus promoting the uptake of LDL-C in the blood. Rebaudioside A can be used for studies on blood glucose and lipid regulation as well as anti-obesity.
    Rebaudioside A (Standard)
  • HY-119695AR
    Simvastatin acid ammonium (Standard)
    Inhibitor
    Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
    Simvastatin acid ammonium (Standard)
Cat. No. Product Name / Synonyms Application Reactivity