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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.
Cat No. product name
T3698 Alpha-Asarone Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
T13131 Tert-Buthyl Pitavastatin tert-Buthyl Pitavastatin is Pitavastatin metabolite. Pitavastatin is a potent inhibitor of HMG-CoA reductase.
T1487 Fluvastatin sodium Fluvastatin sodium, a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.
T0683 Mevastatin Mevastatin is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials....
T1676 Rosuvastatin Rosuvastatin is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversio...
TN1733 Hesperetin 7-O-glucoside Hesperetin 7-O-glucoside and prunin are direct precursors of naringin and neohesperidin, respectively, in C. aurantium. Hesperetin 7-O-glucoside shows inhibition...
T12092 Monacolin J Monacolin J is a cholesterol biosynthesis inhibitor.
T0672 Pravastatin sodium Pravastatin sodium, an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.
T6994 SR12813 SR-12813 is a pregnane X receptor (PXR) agonist.
T20765 Atorvastatin Atorvastatin is an orally active inhibitor of HMG-CoA reductase,is a lipid-lowering agent (human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39...
T26644 Apomine Apomine is an inhibitor of HMG-CoA-reductase. Apomine promotes apoptosis of myeloma cells in vitro and is associated with a modulation of myeloma in vivo. Apomin...
T0687 Simvastatin Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor.
T14342 Atorvastatin lactone Atorvastatin lactone is a prodrug of atorvastatin. Atorvastatin is an orally active inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase.
T1510 Rosuvastatin calcium Rosuvastatin, a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.
T6450 Clinofibrate Clinofibrate(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholesterol an...
T3116 Atorvastatin hemicalcium salt Atorvastatin hemicalcium salt, an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.
T1664 Meglutol Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids. It acts by interfering with the enzymatic st...
T2534 Pitavastatin calcium Pitavastatin 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 hum...
T1207 Lovastatin Lovastatin is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.
T4717 25-Hydroxycholesterol 25-Hydroxycholesterol is a steroid derivative that suppresses the cleavage of sterol regulatory element binding proteins (SREBPs). It inhibits HMG-CoA reductase ...
T11572 HMG499 HMG499 is a potent and selective HMG-CoA reductase inhibitor (IC50: 0.41 μM). HMG499 can prevent the statins-induced accumulation of HMGCR, reduce serum choleste...
T10767 Cerivastatin sodium 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 prol...
T10324 Anhydrosimvastatin Anhydrosimvastatin is an impurity of Simvastatin. Simvastatin is an HMG-CoA reductase inhibitor.
T10070 2'-Ethyl Simvastatin 2'-Ethyl Simvastatin is a Mevinolin analog with HMG-CoA reductase inhibition.
alpha-Asarone
T3698
Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
Tert-Buthyl Pitavastatin
T13131
tert-Buthyl Pitavastatin is Pitavastatin metabolite. Pitavastatin is a potent inhibitor of HMG-CoA reductase.
Fluvastatin sodium
T1487
Fluvastatin sodium, a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.
Mevastatin
T0683
Mevastatin is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials....
Rosuvastatin
T1676
Rosuvastatin is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversio...
Hesperetin 7-O-glucoside
TN1733
Hesperetin 7-O-glucoside and prunin are direct precursors of naringin and neohesperidin, respectively, in C. aurantium. Hesperetin 7-O-glucoside shows inhibition...
Monacolin J
T12092
Monacolin J is a cholesterol biosynthesis inhibitor.
Pravastatin sodium
T0672
Pravastatin sodium, an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.
SR12813
T6994
SR-12813 is a pregnane X receptor (PXR) agonist.
Atorvastatin
T20765
Atorvastatin is an orally active inhibitor of HMG-CoA reductase,is a lipid-lowering agent (human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.3...
Apomine
T26644
Apomine is an inhibitor of HMG-CoA-reductase. Apomine promotes apoptosis of myeloma cells in vitro and is associated with a modulation of myeloma in vivo. Apomin...
Simvastatin
T0687
Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor.
Atorvastatin lactone
T14342
Atorvastatin lactone is a prodrug of atorvastatin. Atorvastatin is an orally active inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase.
Rosuvastatin calcium
T1510
Rosuvastatin, a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.
Clinofibrate
T6450
Clinofibrate(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholestero...
Atorvastatin hemicalcium salt
T3116
Atorvastatin hemicalcium salt, an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.
Meglutol
T1664
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids. It acts by interfering with the enzymatic st...
Pitavastatin calcium
T2534
Pitavastatin 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 hum...
Lovastatin
T1207
Lovastatin is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.
25-Hydroxycholesterol
T4717
25-Hydroxycholesterol is a steroid derivative that suppresses the cleavage of sterol regulatory element binding proteins (SREBPs). It inhibits HMG-CoA reductase ...
HMG499
T11572
HMG499 is a potent and selective HMG-CoA reductase inhibitor (IC50: 0.41 μM). HMG499 can prevent the statins-induced accumulation of HMGCR, reduce serum cholest...
Cerivastatin sodium
T10767
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 prol...
Anhydrosimvastatin
T10324
Anhydrosimvastatin is an impurity of Simvastatin. Simvastatin is an HMG-CoA reductase inhibitor.
2'-Ethyl Simvastatin
T10070
2'-Ethyl Simvastatin is a Mevinolin analog with HMG-CoA reductase inhibition.