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

HMG-CoA Reductase (HMGCR)

HMG-CoA Reductase (HMGCR) is the rate-controlling enzyme of the mevalonate pathway, the metabolic pathway that produces cholesterol and other isoprenoids. Normally in mammalian cells this enzyme is suppressed by cholesterol derived from the internalization and degradation of low density lipoprotein (LDL) via the LDL receptor as well as oxidized species of cholesterol. Competitive inhibitors of the reductase induce the expression of LDL receptors in the liver, which in turn increases the catabolism of plasma LDL and lowers the plasma concentration of cholesterol, an important determinant of atherosclerosis. HMG-CoA reductase is thus the target of the widely available cholesterol-lowering drugs known collectively as the statins. HMG-CoA reductase is anchored in the membrane of the endoplasmic reticulum, and was long regarded as having seven transmembrane domains, with the active site located in a long carboxyl terminal domain in the cytosol.

HMG-CoA Reductase (HMGCR) Related Products (24):

Cat. No. Product Name Effect Purity
  • HY-17502
    Simvastatin Inhibitor 99.81%
    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  • HY-N0504
    Lovastatin Inhibitor 99.47%
    Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
  • HY-17379
    Atorvastatin hemicalcium salt Inhibitor 99.98%
    Atorvastatin hemicalcium salt is a potent HMG-CoA reductase inhibitor with an IC50 value of 8 nM.
  • HY-17504
    Rosuvastatin Calcium Inhibitor
    Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-B0144
    Pitavastatin Calcium Inhibitor 99.94%
    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.
  • HY-14664A
    Fluvastatin sodium Inhibitor >98.0%
    Fluvastatin sodium (XU 62320 sodium) is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), used to treat hypercholesterolemia and to prevent cardiovascular disease.
  • HY-17408
    Mevastatin Inhibitor 99.59%
    Mevastatin (Compactin; ML236B) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans.
  • HY-B0165A
    Pravastatin sodium Inhibitor 99.32%
    Pravastatin (sodium) (CS-514 (sodium)) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
  • HY-100793
    SR12813 Inhibitor 98.04%
    SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.
  • HY-13528
    Clinofibrate Inhibitor >98.0%
    Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor.
  • HY-17640
    Nicodicosapent Inhibitor 98.19%
    Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.
  • HY-14664
    Fluvastatin Inhibitor
    Fluvastatin (XU 62320) inhibits HMG-CoA reductase activity with IC50 of 8 nM.
  • HY-B0144A
    Pitavastatin Inhibitor
    Pitavastatin (NK-104) is a potent HMG-CoA reductase inhibitor, Pitavastatin inhibited cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2).
  • HY-B0589
    Atorvastatin Inhibitor
    Atorvastatin is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol.
  • HY-17504S
    Rosuvastatin D6 Calcium Inhibitor 98.54%
    Rosuvastatin D6 Calcium is deuterium labeled Rosuvastatin, which is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
  • HY-B0165
    Pravastatin Inhibitor
    Pravastatin (CS-514) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
  • HY-114316
    HMG499 Inhibitor
    HMG499 is a potent and selective HMG-CoA reductase inhibitor with an IC50 of 0.41 μM. HMG499 can prevent statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis.
  • HY-104051
    Monacolin J Inhibitor
    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  • HY-B0144AS
    Pitavastatin D4 Inhibitor
    Pitavastatin D4 is deuterium labeled Pitavastatin, which is a potent HMG-CoA reductase inhibitor.
  • HY-17504BS
    Rosuvastatin D3 Sodium Inhibitor
    Rosuvastatin D3 Sodium is deuterium labeled Rosuvastatin, which is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
Isoform Specific Products

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