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HMG-CoA Reductase (HMGCR)

HMG-CoA Reductase (HMGCR) is the rate-controlling enzyme 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, an important determinant of atherosclerosis. HMG-CoA reductase is thus the target of the widely available cholesterol-lowering drugs known collectively as the . 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.

www.MedChemExpress.com 1 HMG-CoA Reductase (HMGCR) Inhibitors & Modulators

Atorvastatin hemicalcium salt Cat. No.: HY-B0589 (CI-981; Atorvastatin hemicalcium) Cat. No.: HY-17379

Bioactivity: Atorvastatin is an inhibitor of HMG-CoA reductase used as a Bioactivity: Atorvastatin hemicalcium salt is a potent HMG-CoA cholesterol-lowering that blocks the production of reductase inhibitor with an IC50 value of 8 nM. cholesterol.

Purity: >98% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Clinofibrate (S-8527) Cat. No.: HY-13528 (XU 62320) Cat. No.: HY-14664

Bioactivity: (S-8527) is a hypelipidemic agent and a Bioactivity: Fluvastatin (XU 62320) inhibits HMG-CoA reductase activity

HMG-CoA reductase inhibitor. with IC 50 of 8 nM.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Fluvastatin D6 sodium Fluvastatin sodium (XU 62320 D6 sodium) Cat. No.: HY-14664AS (XU 62320 sodium) Cat. No.: HY-14664A

Bioactivity: Fluvastatin (XU 62320) D6 sodium is deuterium labeled Bioactivity: Fluvastatin (XU 62320) sodium is a competitive inhibitor of Fluvastatin sodium, which is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), used to hydroxymethylglutaryl-coenzyme A reductase (HMGCR). treat hypercholesterolemia and to prevent cardiovascular disease.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10mM x 1mL in Water, 50 mg, 100 mg

HMG499 Cat. No.: HY-114316 (Mevinolin) Cat. No.: HY-N0504

Bioactivity: HMG499 is a potent and selective HMG-CoA reductase Bioactivity: Lovastatin is a cell-permeable HMG-CoA reductase inhibitor

inhibitor with an IC50 of 0.41 μM. HMG499 can prevent used to lower cholesterol. statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis [1]. Purity: >98% Purity: 99.47% Clinical Data: No Development Reported Clinical Data: Launched Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg

Meglutol (Dicrotalic acid; 3-Hydroxy-3-methylglutaric acid) Cat. No.: HY-B1189 (Compactin; ML236B) Cat. No.: HY-17408

Bioactivity: Meglutol is an antilipemic agent which lowers cholesterol, Bioactivity: Mevastatin (Compactin; ML236B) inhibits HMGCR (HMG-CoA triglycerides, serum beta-lipoproteins and phospholipids, and reductase) (Ki for acid form is 1 nM) which in turn inhibits inhibits the activity of hydroxymethylglutarryl CoA isoprenoid biosynthesis and therefore blocks protein reductases, which is the rate limiting enzyme in the isoprenylation and reduces plasma cholesterol levels in biosynthesis of cholesterol. humans. IC50 value: 1 nM (Ki) Target: HMGCR Mevastatin induces… Purity: >98% Purity: 98.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Monacolin J Nicodicosapent (Antibiotic MB 530A; Lovastatin diol lactone) Cat. No.: HY-104051 Cat. No.: HY-17640

Bioactivity: Monacolin J is an inhibitor of cholesterol biosynthesis, and Bioactivity: Nicodicosapent is a fatty acid conjugate that is also inhibits the activity of HMG-CoA reductase. an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1. Purity: >98% Purity: 98.19% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Pitavastatin Calcium (NK-104) Cat. No.: HY-B0144A (Pitavastatin (hemicalcium); NK-104 (hemicalcium)) Cat. No.: HY-B0144

Bioactivity: Pitavastatin (NK-104) is a potent HMG-CoA reductase inhibitor, Bioactivity: Pitavastatin Calcium is a potent hydroxymethylglutaryl-CoA Pitavastatin inhibited cholesterol synthesis from acetic acid (HMG-CoA) reductase inhibitor. Pitavastatin inhibits with an IC50 of 5.8 nM in a human liver cancer cell line cholesterol synthesis from acetic acid with an IC50 of 5.8 nM (HepG2). in HepG2 cells.

Purity: >98% Purity: 99.94% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Pitavastatin D4 (NK-104 D4) Cat. No.: HY-B0144AS (CS-514) Cat. No.: HY-B0165

Bioactivity: Pitavastatin D4 is deuterium labeled Pitavastatin, which is a Bioactivity: Pravastatin (CS-514) is an HMG-CoA reductase inhibitor against

potent HMG-CoA reductase inhibitor. sterol synthesis with IC 50 of 5.6 μM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mg, 50 mg, 100 mg

Pravastatin sodium (CS-514 (sodium)) Cat. No.: HY-B0165A (ZD 4522) Cat. No.: HY-17504A

Bioactivity: Pravastatin (sodium) (CS-514 (sodium)) is an HMG-CoA reductase Bioactivity: Rosuvastatin is a competitive inhibitor of HMG-CoA reductase

inhibitor against sterol synthesis with IC 50 of 5.6 μM. with IC50 of 11 nM. IC50 Value: 11 nM [1] Target: HMG-CoA reductase in vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C.… Purity: 99.32% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg, 200 mg

Rosuvastatin Calcium Rosuvastatin D3 Sodium (Rosuvastatin hemicalcium; ZD 4522 Calcium) Cat. No.: HY-17504 Cat. No.: HY-17504BS

Bioactivity: Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA Bioactivity: Rosuvastatin D3 Sodium is deuterium labeled Rosuvastatin, reductase with IC50 of 11 nM. IC50 Value: 11 nM [1] Target: which is a competitive inhibitor of HMG-CoA reductase with HMG-CoA reductase in vitro: Rosuvastatin is relatively IC50 of 11 nM. hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion… Purity: 97.73% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg, 100 mg, 200 mg

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Rosuvastatin D6 Calcium Rosuvastatin D6 Sodium Cat. No.: HY-17504S Cat. No.: HY-17504BS1

Bioactivity: Rosuvastatin D6 Calcium is deuterium labeled Rosuvastatin, Bioactivity: Rosuvastatin D6 Sodium is deuterium labeled Rosuvastatin, which is a competitive inhibitor of HMG-CoA reductase with which is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 of 11 nM.

Purity: 98.54% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Simvastatin SR12813 (MK 733) Cat. No.: HY-17502 (GW 485801) Cat. No.: HY-100793

Bioactivity: (MK 733) is a competitive inhibitor of HMG-CoA Bioactivity: SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, reductase with a Ki of 0.2 nM. with an IC 50 value of 0.85 μM.

Purity: 98.0% Purity: 99.04% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]