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-B0144S
    Pitavastatin-d4 hemicalcium
    		Inhibitor
    Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). 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. Anti-cancer activity[1][2][3].
    Pitavastatin-d<sub>4</sub> hemicalcium
  • HY-136347
    3α-Hydroxy pravastatin sodium
    		Inhibitor 99.35%
    3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor.
    3α-Hydroxy pravastatin sodium
  • HY-W707564
    Atorvastatin-d5-1 sodium
    Atorvastatin-d5-1 sodium is the deuterium labeled Atorvastatin sodium (HY-108257). 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-d<sub>5</sub>-1 sodium
  • HY-17379R
    Atorvastatin hemicalcium salt (Standard)
    		Inhibitor
    Atorvastatin (hemicalcium salt) (Standard) is the analytical standard of Atorvastatin (hemicalcium salt). This product is intended for research and analytical applications. Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, 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 (Standard)
  • 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-N6712R
    Thiolutin (Standard)
    		Inhibitor
    Thromycin (Standard) is the analytical standard of thromycin (Acetopyrrothin) (HY-N6712). Thiolutin is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin (HY-15142A)-induced cardiotoxicity (DOXIC)[1][2][3][4][5].
    Thiolutin (Standard)
  • 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-176089
    Adenosine-5'-O-diphosphoribose phosphate sodium
    		Inhibitor
    Adenosine-5'-O-diphosphoribose phosphate sodium is a structural analog of NADPH (HY-113324). Adenosine-5'-O-diphosphoribose phosphate sodium is an HMG-CoA reductase inhibitor. Adenosine-5'-O-diphosphoribose phosphate sodium inhibits microsomal HMG-CoA reductase with an apparent Ki value of 550 μM at low thiol concentrations.
    Adenosine-5'-O-diphosphoribose phosphate sodium
  • HY-N7264R
    7α-Hydroxycholesterol (Standard)
    		Inhibitor
    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 (Standard)
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity