hmg-coa reductase (hmgcr)

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.

Crilvastatin (PMD 387) is a novel, non-competitive hydroxymethylglutaryl coenzyme A reductase inhibitor with cholesterol-lowering activity, inhibiting cholesterol uptake in rats with hereditary hypercholesterolemia.

Lovastatin (MK-803) is an HMG-CoA reductase inhibitor (IC50=3.4 nM). Lovastatin lowers cholesterol and is commonly used as a lipid-lowering agent in the treatment of hypercholesterolemia.

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.

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.

Pravastatin sodium (CS-514 (sodium)), an HMG-CoA reductase inhibitor, inhibits sterol synthesis with IC50 of 5.6 μM.

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.

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.

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.

Cerivastatin is an orally active and highly effective HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects. Cerivastatin can reduce low-density lipoprotein cholesterol levels, inhibit the proliferation and invasion of MDA-MB-231 cells, and can be used to study primary hyperlipidemia.

Fluvastatin sodium (Fluvastatin sodium salt), a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Atorvastatin hemicalcium salt (Atorvastatin Calcium) is an HMG-CoA reductase inhibitor with oral activity. Atorvastatin hemicalcium salt is used to lower cholesterol.

SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.

Atorvastatin, an orally active HMG-CoA reductase inhibitor, effectively lowers blood lipids by activating liver cytochrome p450 to accelerate metabolism. Atorvastatin inhibits the 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.

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

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.

Monacolin J (Antibiotic MB 530A) is a cholesterol biosynthesis inhibitor.

Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor (IC50: 11 nM) that effectively blocks hERG currents (IC50: 195 nM), reduces the expression of mature hERG, and inhibits the interaction of heat shock protein 70 (Hsp70) with hERG protein.

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.

HMG499 is a potent and selective HMG-CoA reductase inhibitor with an IC50 of 0.41 μM, capable of eliminating statins-induced accumulation of HMGCR, lowering serum cholesterol levels, and decreasing atherosclerosis [1].

ent-Atorvastatin is a selective and competitive inhibitor of HMGCR (HMG-CoA reductase).

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.

Pitavastatin (NK-104) is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, effectively inhibiting cholesterol synthesis from acetic acid in HepG2 cells with an IC50 of 5.8 nM. It also induces hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptors and exhibits therapeutic activities such as anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective, and reno-protective effects.