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Metabolism HMG-CoA Reductase

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
T0672 Pravastatin sodium Pravastatin sodium, an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.
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...
T0687 Simvastatin Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor.
T1207 Lovastatin Lovastatin is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.
T1487 Fluvastatin sodium salt Fluvastatin sodium, a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.
T1510 Rosuvastatin calcium Rosuvastatin, a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.
T1664 Meglutol Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids. It acts by interfering with the enzymatic s...
T1676 Rosuvastatin Rosuvastatin is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversi...
T3116 Atorvastatin Calcium Atorvastatin hemicalcium salt, an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.
T3698 alpha-Asarone Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
T6450 Clinofibrate Clinofibrate(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholester...
T6994 SR-12813 SR-12813 is a pregnane X receptor (PXR) agonist.
T4717 25-Hydroxycholesterol 25-Hydroxycholesterol is a steroid derivative that suppresses the cleavage of sterol regulatory element binding proteins (SREBPs). It inhibits HMG-CoA reductas...
TN1377 alpha-Spinasterol Alpha-Spinasterol is a novel efficacious and safe antagonist of the TRPV1 receptor with anti-inflammatory and antinociceptive effects.
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 inhibitio...
TN2111 Prunin Prunin possesses anti-diabetic, and anti-abacterial properties, it can inhibit protein tyrosine phosphatase 1B (PTP1B) and stimulate glucose uptake in insulin-r...
T12092 Monacolin J Monacolin J is a cholesterol biosynthesis inhibitor.
T10070 2'-Ethyl Simvastatin 2'-Ethyl Simvastatin is a Mevinolin analog with HMG-CoA reductase inhibition.
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....
T11572 HMG499 HMG499 can prevent statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis. HMG499 is a potent and selective HMG-Co...
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 pro...
Pravastatin sodium
T0672CAS 81131-70-6
Pravastatin sodium, an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.
Mevastatin
T0683CAS 73573-88-3
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...
Simvastatin
T0687CAS 79902-63-9
Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor.
Lovastatin
T1207CAS 75330-75-5
Lovastatin is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.
Fluvastatin sodium salt
T1487CAS 93957-55-2
Fluvastatin sodium, a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.
Rosuvastatin calcium
T1510CAS 147098-20-2
Rosuvastatin, a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.
Meglutol
T1664CAS 503-49-1
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids. It acts by interfering with the enzymatic s...
Rosuvastatin
T1676CAS 287714-41-4
Rosuvastatin is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversi...
Atorvastatin Calcium
T3116CAS 134523-03-8
Atorvastatin hemicalcium salt, an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.
alpha-Asarone
T3698CAS 2883-98-9
Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
Clinofibrate
T6450CAS 30299-08-2
Clinofibrate(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholester...
SR-12813
T6994CAS 126411-39-0
SR-12813 is a pregnane X receptor (PXR) agonist.
25-Hydroxycholesterol
T4717CAS 2140-46-7
25-Hydroxycholesterol is a steroid derivative that suppresses the cleavage of sterol regulatory element binding proteins (SREBPs). It inhibits HMG-CoA reductas...
alpha-Spinasterol
TN1377CAS 481-18-5
Alpha-Spinasterol is a novel efficacious and safe antagonist of the TRPV1 receptor with anti-inflammatory and antinociceptive effects.
Hesperetin 7-O-glucoside
TN1733CAS 31712-49-9
Hesperetin 7-O-glucoside and prunin are direct precursors of naringin and neohesperidin, respectively, in C. aurantium. Hesperetin 7-O-glucoside shows inhibitio...
Prunin
TN2111CAS 529-55-5
Prunin possesses anti-diabetic, and anti-abacterial properties, it can inhibit protein tyrosine phosphatase 1B (PTP1B) and stimulate glucose uptake in insulin-r...
Monacolin J
T12092CAS 79952-42-4
Monacolin J is a cholesterol biosynthesis inhibitor.
2'-Ethyl Simvastatin
T10070CAS 79902-42-4
2'-Ethyl Simvastatin is a Mevinolin analog with HMG-CoA reductase inhibition.
Atorvastatin 
T20765CAS 134523-00-5
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....
HMG499
T11572CAS
HMG499 can prevent statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis. HMG499 is a potent and selective HMG-Co...
Cerivastatin sodium
T10767CAS 143201-11-0
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 pro...