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-139134
    S-2E
    		Inhibitor
    S-2E is an orally active and noncompetitive HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. S-2E has an anti-hyperlipidemic action. S-2E has the potential for familial hypercholesterolemia and mixed hyperlipidemia research.
    S-2E
  • HY-B0144AS3
    Pitavastatin-d4-1 sodium
    		99.22%
    Pitavastatin-d4-1 (NK-104-d4-1) sodium is the deuterium labeled Pitavastatin sodium (HY-B0144B). 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-d<sub>4</sub>-1 sodium
  • HY-135405R
    4-Acetylsimvastatin (Standard)
    		Inhibitor
    4-Acetylsimvastatin (Standard) is the analytical standard of 4-Acetylsimvastatin. This product is intended for research and analytical applications. 4-Acetylsimvastatin is an acetylated simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
    4-Acetylsimvastatin (Standard)
  • HY-137390A
    (3S,5R)-Fluvastatin potassium
    (3S,5R)-Fluvastatin (potassium) is a synthetic hypolipidemic drug that inhibits HMG-CoA reductase activity. (3S,5R)-Fluvastatin (potassium) has similar antioxidative effects on copper ion-induced LDL oxidation compared to its 3R,5S enantiomer. (3S,5R)-Fluvastatin (potassium) and its metabolites demonstrate a potential to exhibit anti-atherosclerotic effects through their antioxidative activities. (3S,5R)-Fluvastatin (potassium) is clinically utilized as part of a racemic mixture for reducing plasma cholesterol levels.
    (3S,5R)-Fluvastatin potassium
  • HY-116241
    L-157012
    		Inhibitor
    L-157012 is a HMG-CoA reductase (HMGCR) inhibitor. L-157012 is also a cholesterol-lowering agent.
    L-157012
  • HY-17504AS
    Rosuvastatin-d3
    		Inhibitor
    Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin 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-d<sub>3</sub>
  • HY-17504C
    (3R,5R)-Rosuvastatin
    		Inhibitor
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    (3R,5R)-Rosuvastatin
  • HY-19077
    BMS-180431
    		Inhibitor
    BMS-180431 is an inhibitor of HMG-CoA reductase (IC50: 43 nM).
    BMS-180431
  • HY-129149
    Ganoderic acid SZ
    Ganoderic acid SZ is a natural product with 3-hydroxy-3-methylglutaryl-CoA reductase inhibitory activity. Ganoderic acid SZ shows stronger activity than the positive control atorvastatin in inhibiting HMG-CoA reductase. Ganoderic acid SZ exhibits significant inhibition of yeast-derived α-glucosidase with IC50 values achieved at very low concentrations. Ganoderic acid SZ also exhibits cytotoxicity against K562 cells with IC?? values in the range of 10-20 μM.
    Ganoderic acid SZ
  • HY-149310
    Dim16
    		Inhibitor
    Dim16 is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC50 of 0.8 nM against human PCSK9 and an IC50 of 146.8 μM against HMG-CoAR. Dim16 disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 can be used in research related to hypercholesterolemia.
    Dim16
  • HY-N10076
    Ganomycin I
    		Inhibitor
    Ganomycin I is a dual inhibitor of α-Glucosidase and HMG-CoA reductase. Ganomycin I can also inhibits HIV protease. Ganomycin I exhibits anti-diabetic and anti-osteoclastogenesis effects.
    Ganomycin I
  • HY-101873S
    Atorvastatin lactone-d5
    		Inhibitor
    Atorvastatin lactone-d5 is a deuterated form of Atorvastatin lactone (HY-101873). Atorvastatin lactone is a proagent form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
    Atorvastatin lactone-d<sub>5</sub>
  • HY-RS06239
    Hmgcr Mouse Pre-designed siRNA Set A
    		Inhibitor

    Hmgcr Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hmgcr gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Hmgcr Mouse Pre-designed siRNA Set A
  • HY-135405
    4-Acetylsimvastatin
    		Inhibitor
    4-Acetylsimvastatin is an acetylated simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
    4-Acetylsimvastatin
  • HY-17502S
    Simvastatin-d11
    Simvastatin-d11 is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
    Simvastatin-d<sub>11</sub>
  • HY-19077A
    BMS-180431 sodium
    		Inhibitor
    BMS-180431 sodium is an inhibitor of HMG-CoA reductase (IC50: 43 nM).
    BMS-180431 sodium
  • HY-119064
    L-645164
    		Inhibitor
    L-645164 is a potent inhibitor of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase. L-645164 produces substantial decreases in circulating serum cholesterol concentrations in dogs. L-645164 is promising for research of central nervous system disorders.
    L-645164
  • HY-N0504S1
    Lovastatin-d9 (epimer mixture)
    		Inhibitor 99.04%
    Lovastatin-d9 is the deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Lovastatin-d<sub>9</sub> (epimer mixture)
  • HY-147195
    QH536
    		Inhibitor
    QH536 (Compound 29) is a potent HMGCR degrader with an EC50 of 0.22 μM. QH536 has no side-effect of inducing cholesterol accumulation in cells. QH536 shows anti-inflammatory and can be used for cardiovascular disease and nonalcoholic steatohepatitis research.
    QH536
  • HY-B0165AS
    Pravastatin-13C,d3 sodium
    		Inhibitor
    Pravastatin-13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin-<sup>13</sup>C,d<sub>3</sub> sodium
Cat. No. Product Name / Synonyms Application Reactivity