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HMG-CoA Reductase

HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-coenzyme A reductase, officially abbreviated HMGCR) is the rate-controlling enzyme (NADH-dependent, ; NADPH-dependent,) of the mevalonate pathway, the metabolic pathway that produces cholesterol and other isoprenoids. Normally in mammalian cells this enzyme is suppressed by cholesterol derived from the internalization and degradation of low density lipoprotein (LDL) via the LDL receptor as well as oxidized species of cholesterol. Competitive inhibitors of the reductase induce the expression of LDL receptors in the liver, which in turn increases the catabolism of plasma LDL and lowers the plasma concentration of cholesterol, which is considered, by those who accept the standard lipid hypothesis, an important determinant of atherosclerosis. This enzyme is thus the target of the widely available cholesterol-lowering drugs known collectively as the statins.HMG-CoA reductase is anchored in the membrane of the endoplasmic reticulum, and was long regarded as having seven transmembrane domains, with the active site located in a long carboxyl terminal domain in the cytosol. More recent evidence shows it to contain eight transmembrane domains.

  • Apomine
    T26644126411-13-0In house
    Apomine (SR-9223i), an inhibitor of HMG-CoA-reductase, promotes apoptosis of myeloma cells in vitro and has been implicated in the regulation of myeloma in vivo. Apomine accelerates the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase and stimulates low-density lipoprotein receptor activity. Apomine enhances the antitumor effect of lovastatin on myeloma cells by downregulating 3-hydroxy-3-methylglutaryl-CoA reductase.
    • $123
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  • Crilvastatin
    T25276120551-59-9In house
    Crilvastatin (PMD 387) is a novel non-competitive hydroxymethylglutaryl coenzyme A reductase inhibitor with cholesterol-lowering activity that inhibits cholesterol uptake in rats with hereditary hypercholesterolemia.
    • $293 TargetMol
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  • Anhydrosimvastatin
    T10324210980-68-0
    Anhydrosimvastatin (Dehydro simvastatin) is an impurity of Simvastatin. Simvastatin is an HMG-CoA reductase inhibitor.
    • $232
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    TargetMol | Inhibitor Sale
  • Atorvastatin Sodium
    T20887134523-01-6In house
    Atorvastatin Sodium (Lipitor) is a competitive inhibitor of HMG-CoA reductase and increases the expression of low density lipoprotein (LDL) receptors on hepatocytes. Atorvastatin Sodium treatment inhibits aquaporin 4 to reduce ischaemic brain oedema.
    • $50
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  • Tenivastatin
    T24865121009-77-6In house
    Tenivastatin (Simvastatin acid) is an anti-hyperlipidemic HMG-CoA reductase inhibitor that inhibits the production of reactive oxygen species (ROS) and can be used in the study of primary hyperlipidemia.
    • $350 TargetMol
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  • Dalvastatin
    T25285132100-55-1In house
    Dalvastatin (RG-12561) is an orally available inhibitor of HMG-CoA reductase and cholesterol-lowering synthesis.Dalvastatin competitively inhibits rat hepatic HMG-CoA reductase with an IC50 value of 3.4 nmol / l. Dalvastatin inhibits cholesterol biosynthesis in liver sections in rat experiments with an ED50 value of 0.9.
    • $191
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  • Lovastatin
    T120775330-75-5
    Lovastatin (MK-803) is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.
    • $34
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    TargetMol | Citations Cited
  • Pravastatin sodium
    T067281131-70-6
    Pravastatin sodium (CS-514 (sodium)), an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.
    • $40
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  • Fluvastatin sodium
    T148793957-55-2
    Fluvastatin sodium (Fluvastatin sodium salt), a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.
    • $30
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  • Rosuvastatin
    T1676287714-41-4
    Rosuvastatin (ZD 4522) is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
    • $45
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  • Atorvastatin
    T20765134523-00-5
    Atorvastatin is an orally active HMG-CoA reductase inhibitor that has the ability to effectively lower blood lipids by activating liver cytochrome p450 to accelerate metabolism. Atorvastatin inhibited proliferation and invasion of human SV-SMC cells with IC50 values of 0.39 μM and 2.39 μM, respectively. Atorvastatin combined with clopidogrel may lead to increased thrombotic events in patients.
    • $29
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  • 25-Hydroxycholesterol
    T47172140-46-7
    25-Hydroxycholesterol is a steroid derivative that suppresses the cleavage of sterol regulatory element binding proteins (SREBPs). It inhibits HMG-CoA reductase and so it also plays a significant role in the in vivo regulation of cholesterol biosynthesis
    • $45
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  • SR12813
    T6994126411-39-0
    SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.
    • $50
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  • Cerivastatin sodium
    T10767143201-11-0
    Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM). It also inhibits the proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition.
    • $67
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  • Pitavastatin calcium
    T2534147526-32-7
    Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.
    • $34
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  • Rosuvastatin calcium
    T1510147098-20-2
    Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.
    • $34
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    TargetMol | Citations Cited
  • Simvastatin
    T068779902-63-9
    Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.
    • $36
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  • Tert-Buthyl Pitavastatin
    T13131586966-54-3
    tert-Buthyl Pitavastatin is Pitavastatin metabolite. Pitavastatin is a potent inhibitor of HMG-CoA reductase.
    • $42
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  • Meglutol
    T1664503-49-1
    Meglutol (3-Hydroxy-3-methylglutaric acid) is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids. It acts by interfering with the enzymatic steps involved in the conversion of acetate to hydroxymethyl glutaryl coenzyme A as well as inhibiting the activity of HYDROXYMETHYLGLUTARYL COA REDUCTASES which is the rate-limiting enzyme in the biosynthesis of cholesterol.
    • $45
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  • alpha-Asarone
    T36982883-98-9
    alpha-Asarone (trans-Asarone) is a psychoactive compound with antidepressant-like activity in mice.
    • $30
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  • Monacolin J
    T1209279952-42-4
    Monacolin J (Antibiotic MB 530A) is a cholesterol biosynthesis inhibitor.
    • $72
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  • Clinofibrate
    T645030299-08-2
    Clinofibrate (Lipoclin)(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholesterol and triacylglyceride levels in the blood.
    • $39
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  • Fluvastatin
    T2140593957-54-1
    Fluvastatin (XU-62320) is a potent and competitive HMG-CoA reductase inhibitor (IC50: 8 nM) that inhibits oxidative stress in vascular smooth muscle cells through an Nrf2-dependent pathway, and is used for the reduction of plasma cholesterol levels and the prevention of cardiovascular disease.
    • $30
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  • Mevastatin
    T068373573-88-3
    Mevastatin (ML236B) is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials.
    • $51
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  • beta-Amyrin acetate
    TN14381616-93-9
    beta-Amyrin acetate inhibits HMG-CoA Reductase (HMGCR) and sEH activity with IC50 of 3.4 μM. beta-Amyrin acetate has anti-inflammatory, antifungal, antioxidant, and anti-hyperlipidemic activities.
    • $68
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  • Atorvastatin hemicalcium salt
    T3116134523-03-8
    Atorvastatin hemicalcium salt (Atorvastatin Calcium), an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.
    • $45
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  • 2'-Ethyl Simvastatin
    T1007079902-42-4
    2'-Ethyl Simvastatin is a Mevinolin analog with HMG-CoA reductase inhibition.
    • $1,520
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  • HMG499
    T115722416941-68-7
    HMG499 is a potent and selective HMG-CoA reductase inhibitor with an IC 50 of 0.41 μM. HMG499 can eliminate statins-induced accumulation of HMGCR, lower serum cholesterol levels and decrease atherosclerosis [1].
    • $2,140
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  • Pitavastatin lactone
    T12490141750-63-2
    Pitavastatin lactone is the major metabolite of Pitavastatin in humans.Pitavastatin is a competitive inhibitor of HMG-CoA reductase.
    • $66
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  • Pitavastatin
    T7072147511-69-1
    Pitavastatin (NK-104) is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor with hypocholesterolemic and neuroprotective activities, inhibits synthesis of cholesterol from acetic acid, and reduces oxidative stress.Pitavastatin is a hepatocellular low-density lipoprotein cholesterol (LDL-C) receptor inducer, and may be used to Pitavastatin is a hepatocellular LDL-C receptor inducer and is used in the study of coronary atherosclerosis, hypercholesterolemia, and acute coronary syndromes.Pitavastatin is structurally unstable and is recommended to be formulated for immediate use.
    • $970
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  • Hesperetin 7-O-glucoside
    TN173331712-49-9
    Hesperetin 7-O-glucoside and prunin are direct precursors of naringin and neohesperidin, respectively, in C. aurantium. Hesperetin 7-O-glucoside shows inhibition of human HMG-CoA reductase, it also exhibits effective inhibition of the growth of Helicobacter pylori. Hesperetin 7-O-glucoside can reduce blood pressure in healthy volunteers.
    • $89
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  • Atorvastatin lactone
    T14342125995-03-1
    Atorvastatin lactone is a prodrug form of atorvastatin. Which is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
    • $32
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