hmg-coa reductase (hmgcr)

HMG-CoA Reductase-IN-1 is an inhibitor of HMG-CoA reductase, demonstrating strong inhibitory activity on HMGR and affinity for OATP1B1, with pIC50 and pKm values of 8.54 and 1.98, respectively. It is utilized in hypercholesterolemia research [1].

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

Lovastatin (MK-803) is an HMG-CoA Reductase Inhibitor, used for lowering cholesterol.

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

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

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.

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.

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

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.

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.

Ganoderenic Acid K, isolated from the fruiting bodies of Ganoderma lucidum, exhibits potent inhibitory activity against HMG-CoA reductase (HMGCR), demonstrating an IC50 of 16.5 μM [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.

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

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

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.

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.

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.

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

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].

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.

Simvastatin acid (Tenivastatin) calcium hydrate is an orally active inhibitor of HMG-CoA reductase (HMGCR). Simvastatin acid calcium hydrate also inhibits indoxyl sulfate mediated reactive oxygen species (ROS) production.

Atorvastatin lactone is a prodrug form of atorvastatin. Which is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.

Atorvastatin hemicalcium salt (Atorvastatin Calcium), an effective HMG-CoA reductase inhibitor (IC50 = 8 nM), is utilized as a cholesterol-lowering medication.

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