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-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[1].
    (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-16166
    Dalvastatin
    Dalvastatin (RG-12561) inhibitor of HMG-CoA reductase and cholesterol-lowering synthesis.
    Dalvastatin
  • 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[1].
    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-135383A
    (3S,5R)-Pitavastatin calcium
    Control
    (3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
    (3S,5R)-Pitavastatin calcium
  • 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-135383B
    (Z)-Pitavastatin calcium
    Control
    (Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
    (Z)-Pitavastatin calcium
  • HY-17504BS2
    Rosuvastatin-13C,d3 sodium
    Inhibitor
    Rosuvastatin-13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). 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-<sub>13</sub>C,d<sub>3</sub> sodium
  • 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-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-112490R
    Atorvastatin (calcium hydrate) (Standard)
    Inhibitor
    Atorvastatin (calcium hydrate) (Standard) is the analytical standard of Atorvastatin (calcium hydrate). This product is intended for research and analytical applications. Atorvastatin calcium salt trihydrate is a drug belonging to the statin class of drugs used to lower blood cholesterol levels. Atorvastatin calcium salt trihydrate has unique chemical properties that make it an effective tool in controlling high levels of low-density lipoprotein (LDL) cholesterol and triglycerides in the body, reducing the risk of heart attack and stroke. Atorvastatin calcium salt trihydrate works by inhibiting HMG-CoA reductase, the enzyme responsible for producing cholesterol in the liver.
    Atorvastatin (calcium hydrate) (Standard)
  • HY-17504AS1
    Rosuvastatin-d6
    Inhibitor
    Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks 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 reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin-d<sub>6</sub>
Cat. No. Product Name / Synonyms Application Reactivity