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-B0589
    Atorvastatin
    Inhibitor 99.72%
    Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin
  • HY-17502
    Simvastatin
    Inhibitor 99.56%
    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
    Simvastatin
  • HY-N0504
    Lovastatin
    Inhibitor 99.75%
    Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Lovastatin
  • HY-17504
    Rosuvastatin Calcium
    Inhibitor 99.77%
    Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin Calcium
  • HY-B0144A
    Pitavastatin
    Inhibitor 98.87%
    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
  • HY-108744
    Pitavastatin magnesium
    Inhibitor 99.76%
    Pitavastatin magnesium is an orally active HMG-CoA Reductase inhibitor. Pitavastatin magnesium lowers total cholesterol and low-density lipoprotein cholesterol in a hyperlipidemic rat model. Pitavastatin magnesium can be used in research on cardiovascular and cerebrovascular diseases such as hyperlipidemia.
    Pitavastatin magnesium
  • HY-171823
    PROTAC HMGCR Degrader-1
    Degrader
    PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research.
    PROTAC HMGCR Degrader-1
  • HY-182257
    Atorvastatin (lysine)
    Inhibitor
    Atorvastatin lysine is an inhibitor of HMG-CoA reductase. Atorvastatin lysine can be used to study hypercholesterolemia and mixed hyperlipidemia.
    Atorvastatin (lysine)
  • HY-B0165A
    Pravastatin sodium
    Inhibitor 99.38%
    Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin sodium
  • HY-14664
    Fluvastatin
    Inhibitor 98.49%
    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
  • HY-17379
    Atorvastatin hemicalcium salt
    Inhibitor 99.94%
    Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, with blood-brain barrier permeability. Atorvastatin hemicalcium salt has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin hemicalcium salt
  • HY-17408
    Mevastatin
    Inhibitor 99.46%
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.
    Mevastatin
  • HY-14664A
    Fluvastatin sodium
    Inhibitor 99.94%
    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
  • HY-B0144
    Pitavastatin Calcium
    Inhibitor 99.89%
    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
  • HY-112490
    Atorvastatin calcium hydrate
    Inhibitor 99.83%
    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
  • HY-N7264
    7α-Hydroxycholesterol
    Inhibitor 99.99%
    7α-Hydroxycholesterol is a cholesterol oxide and can serve as a biomarker for oxidative stress and lipid peroxidation. 7α-Hydroxycholesterol has cytotoxic and pro-inflammatory activities. 7α-Hydroxycholesterol can also inhibit sterol synthesis and reduce the activity of HMG-CoA reductase. 7α-Hydroxycholesterol can be used in the research of diseases such as diabetes and atherosclerosis.
    7α-Hydroxycholesterol
  • HY-17504A
    Rosuvastatin
    Inhibitor 99.67%
    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
  • HY-109523
    Cerivastatin sodium
    Inhibitor 99.89%
    Cerivastatin sodium 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 sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
    Cerivastatin sodium
  • HY-17504B
    Rosuvastatin Sodium
    Inhibitor 99.91%
    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
  • HY-100793
    SR12813
    Inhibitor 99.84%
    SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR).
    SR12813
Cat. No. Product Name / Synonyms Application Reactivity