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

HMG-CoA Reductase (HMGCR)

HMG-CoA Reductase (HMGCR)

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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-129458
    Cerivastatin
    		Inhibitor
    Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
    Cerivastatin
  • HY-113725
    L 668411
    		Inhibitor
    L 668411 is a β-lactone inhibitor with activity against 3-hydroxy-3-methylglutaryl-CoA synthase and cholesterol biosynthesis. L 668411 inhibits rat liver cytosolic 3-hydroxy-3-methylglutaryl-CoA synthase and [14C] acetate incorporation into sterols in cultured Hep G2 cells, and the inhibition appears to be irreversible in cells but reversible in cultured cells and animals.
    L 668411
  • HY-119695AS1
    Simvastatin acid-d9 ammonium
    		Inhibitor
    Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). 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-d<sub>9</sub> ammonium
  • HY-137310
    4-Hydroxy atorvastatin hemicalcium
    4-Hydroxy atorvastatin hemicalcium is a metabolite of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin is metabolized by the cytochrome P450 (CYP) isoform CYP3A4 to form 4-hydroxy atorvastatin.
    4-Hydroxy atorvastatin hemicalcium
  • HY-14664CS
    (3S,5R)-Fluvastatin-d6 sodium
    		Inhibitor ≥98.0%
    (3S,5R)-Fluvastatin-d6 (sodium)?is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin 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.
    (3S,5R)-Fluvastatin-d<sub>6</sub> sodium
  • HY-14664AR
    Fluvastatin sodium (Standard)
    		Inhibitor
    Fluvastatin (sodium) (Standard) is the analytical standard of Fluvastatin (sodium). This product is intended for research and analytical applications. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
    Fluvastatin sodium (Standard)
  • HY-137213
    Fluvastatin lactone
    		Control
    Fluvastatin lactone, a lactone form of Fluvastatin (HY-14664), induces myotoxicity in human skeletal muscle cells.
    Fluvastatin lactone
  • HY-Z8472
    Dihydromevinolin
    		Inhibitor
    Dihydromevinolin is a potent hypocholesterolemic metabolite produced by Aspergillus terreus. Dihydromevinolin is a HMG-CoA reductase inhibitor.
    Dihydromevinolin
  • HY-119695AS2
    Simvastatin acid-d3 ammonium
    		Inhibitor
    Simvastatin acid-d3 (Tenivastatin-d3) ammonium is deuterium-labeled Simvastatin acid (ammonium) (HY-119695A).
    Simvastatin acid-d<sub>3</sub> ammonium
  • HY-13528R
    Clinofibrate (Standard)
    		Inhibitor
    Clinofibrate (Standard) is the analytical standard of Clinofibrate. This product is intended for research and analytical applications. Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor.
    Clinofibrate (Standard)
  • HY-16166
    Dalvastatin
    Dalvastatin (RG-12561) inhibitor of HMG-CoA reductase and cholesterol-lowering synthesis.
    Dalvastatin
  • 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-117780
    Rawsonol
    		Inhibitor
    Rawsonol is a brominated diphenylmethane derivative obtained from the green alga Avrainuika rawsoni. Rawsonol exhibits inhibitory activity against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with activities related to cholesterol biosynthesis inhibition or other metabolic pathways involving HMG-CoA reductase activity.
    Rawsonol
  • 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-B0165CS
    Pravastatin-d3 sodium
    		Inhibitor 99.02%
    Pravastatin-d3 (sodium) is the deuterium labeled Pravastatin sodium salt. Pravastatin (CS-514) sodium salt is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin-d<sub>3</sub> sodium
  • HY-135383A
    (3S,5R)-Pitavastatin calcium
    		Control
    (3S,5R)-Pitavastatin calcium is the enantiomer of Pitavastatin Calcium (HY-B0144). Pitavastatin is a potent HMG-CoA reductase inhibitor.
    (3S,5R)-Pitavastatin calcium
Cat. No. Product Name / Synonyms Application Reactivity