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 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.


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Simvastatin-d3

Simvastatin-d3 is the deuterium labeled Simvastatin[1]. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[2].

  • CAS Number: 1002347-61-6
  • MF: C25H35D3O5
  • MW: 421.58500
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Simvastatin Hydroxy Acid Sodium Salt

Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM[1][2].

  • CAS Number: 101314-97-0
  • MF: C25H39NaO6
  • MW: 458.563
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

beta-Amyrin palmitate

β-Amyrin palmitate shows HMG-CoA reductase inhibition[1]. And β-Amyrin palmitate has anti-diabetes mellitus activity[2].

  • CAS Number: 5973-06-8
  • MF: C46H80O2
  • MW: 665.13
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 661.4±54.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 354.1±18.8 °C

2'-Ethyl Simvastatin

2'-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition[1].

  • CAS Number: 79902-42-4
  • MF: C23H34O5
  • MW: 390.51300
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pravastatin (sodium)

Pravastatin sodium is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.Target: HMG-CoA reductasePravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.

  • CAS Number: 81131-70-6
  • MF: C23H35NaO7
  • MW: 446.51
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: 634.5ºCat 760 mmHg
  • Melting Point: 171.2-173 °C
  • Flash Point: 213.2ºC

Lovastatin

Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.

  • CAS Number: 75330-75-5
  • MF: C24H36O5
  • MW: 404.540
  • Catalog: Ferroptosis
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 559.2±50.0 °C at 760 mmHg
  • Melting Point: 175°C
  • Flash Point: 185.3±23.6 °C

L 669262

L-669,262, a potent inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with an IC50 of 0.10 ng/mL for rat liver HMG-CoA[1].

  • CAS Number: 130468-11-0
  • MF: C25H36O6
  • MW: 432.55
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.16g/cm3
  • Boiling Point: 609.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 202.1ºC

Cerivastatin

Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2][3].

  • CAS Number: 145599-86-6
  • MF: C26H34FNO5
  • MW: 441.53500
  • Catalog: Ferroptosis
  • Density: 1.181 g/cm3
  • Boiling Point: 646.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 344.7ºC

Mevastatin

Mevastatin (Compactin; ML236B) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans. IC50 value: 1 nM (Ki)Target: HMGCRMevastatin induces apoptosis, arrests cancer cells in G1 phase and downregulates cdk 2, 4, and 6, cyclin D1 and E1, p21 and p27. Mevastatin suppresses TNF-induced NF-κB activation (IC50 = ~17 uM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.

  • CAS Number: 73573-88-3
  • MF: C23H34O5
  • MW: 390.513
  • Catalog: Autophagy
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 555.0±50.0 °C at 760 mmHg
  • Melting Point: 151-153 °C
  • Flash Point: 186.5±23.6 °C

Lovastatin hydroxy acid sodium

Lovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM[1].

  • CAS Number: 75225-50-2
  • MF: C24H37NaO6
  • MW: 444.537
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: 602.3ºC at 760 mmHg
  • Melting Point: 154-160ºC
  • Flash Point: 199.1ºC

Lovastatin-d3

Lovastatin-d3 is deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.

  • CAS Number: 1002345-93-8
  • MF: C24H33D3O5
  • MW: 407.56
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

beta-Amyrin acetate

β-Amyrin acetate is a triterpenoid with potent anti-inflammatory, antifungal, anti-diabetic, anti-hyperlipidemic activities. β-Amyrin acetate can inhibit HMG-CoA reductase activity by locating in the hydrophobic binding cleft of HMG CoA reductase[1][2][3][4].

  • CAS Number: 1616-93-9
  • MF: C32H52O2
  • MW: 468.754
  • Catalog: Fungal
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 505.1±49.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 256.2±17.4 °C

LOVASTATIN HYDROXY ACID, SODIUM SALT

Lovastatin acid (Mevinolinic acid), an active metabolite of Lovastatin, is a potent competitive HMG-CoA reductase inhibitor with a Ki of 0.6 nM[1].

  • CAS Number: 75225-51-3
  • MF: C24H38O6
  • MW: 422.55
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.14g/cm3
  • Boiling Point: 602.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 199.1ºC

3-Hydroxy-3-(2H3)methylpentanedioic acid

Meglutol-d3 is the deuterium labeled Meglutol[1]. Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.

  • CAS Number: 59060-36-5
  • MF: C6H7D3O5
  • MW: 165.159
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 354.3±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 182.2±21.6 °C

Pitavastatin sodium

Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects[1][2][3][8].

  • CAS Number: 574705-92-3
  • MF: C25H23FNNaO4
  • MW: 443.44300
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rosuvastatin D3

Rosuvastatin D3 (ZD 4522 D3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].

  • CAS Number: 1133429-16-9
  • MF: C22H25D3FN3O6S
  • MW: 484.56
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Atorvastatin Sodium

Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3][4][5].

  • CAS Number: 134523-01-6
  • MF: C33H34FN2NaO5
  • MW: 580.62
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 722.2±60.0ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 390.6±32.9ºC

Pitavastatin calcium

Pitavastatin Calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.

  • CAS Number: 147526-32-7
  • MF: C25H23FNO4.1/2Ca
  • MW: 440.49
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 692ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 372.3ºC

Pravastatin

Pravastatin is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.Target: HMG-CoA reductasePravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.

  • CAS Number: 81093-37-0
  • MF: C23H36O7
  • MW: 424.53
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 634.5±55.0 °C at 760 mmHg
  • Melting Point: 171.2-173ºC
  • Flash Point: 213.2±25.0 °C

(rel)-Atorvastatin

(rel)-Atorvastatin, a relative configuration of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3].

  • CAS Number: 110862-48-1
  • MF: C33H35FN2O5
  • MW: 558.640
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 722.2±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 390.6±32.9 °C

(Rac)-5-Keto Fluvastatin

(Rac)-5-Keto Fluvastatin (3-Hydroxy-5-Keto Fluvastatin) is an impurity of Fluvastatin (XU 62320). Fluvastatin is a HMG-CoA reductase inhibitor with an IC50 of 8 nM[1].

  • CAS Number: 1160169-39-0
  • MF: C24H24FNO4
  • MW: 409.45000
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(3R,5S)-Fluvastatin

(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1][2][3].

  • CAS Number: 155229-75-7
  • MF: C24H26FNO4
  • MW: 433.44800
  • Catalog: Autophagy
  • Density: 1.23
  • Boiling Point: 681.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 366.1ºC

Pravastatin Lactone

Pravastatin lactone is a potent HMG-CoA inhibitor. Pravastatin Lactone is a metabolite of pravastatin. Pravastatin lactone reduces blood cholesterol levels by inhibiting cholesterol synthesis[1].

  • CAS Number: 85956-22-5
  • MF: C23H34O6
  • MW: 406.51
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 590.5±50.0 °C at 760 mmHg
  • Melting Point: 140-143ºC
  • Flash Point: 199.5±23.6 °C

Crilvastatin

Crilvastatin (PMD 387) is a potent inhibitor of HMG-CoA reductase[1].

  • CAS Number: 120551-59-9
  • MF: C14H23NO3
  • MW: 253.33700
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.09g/cm3
  • Boiling Point: 389.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 189.6ºC

Lovastatin Diol Lactone

Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.

  • CAS Number: 79952-42-4
  • MF: C19H28O4
  • MW: 320.423
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 535.7±50.0 °C at 760 mmHg
  • Melting Point: 104-114 °C
  • Flash Point: 191.2±23.6 °C

(3R,5R)-Rosuvastatin

(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM[2]. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[3].

  • CAS Number: 1094100-06-7
  • MF: C22H28FN3O6S
  • MW: 481.53800
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Simvastatin acid calcium hydrate

Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1][2].

  • CAS Number: 530112-57-3
  • MF: C50H84CaO15
  • MW: 965.27100
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rosuvastatin Calcium

Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein 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. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].

  • CAS Number: 147098-20-2
  • MF: C22H27Ca0.5FN3O6S
  • MW: 500.57
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: 745.6ºC at 760 mmHg
  • Melting Point: 122ºC
  • Flash Point: 404.7ºC

Simvastatin

Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.

  • CAS Number: 79902-63-9
  • MF: C25H38O5
  • MW: 418.566
  • Catalog: Autophagy
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 564.9±50.0 °C at 760 mmHg
  • Melting Point: 139 °C
  • Flash Point: 184.8±23.6 °C

(3S,5R)-Fluvastatin sodium

(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].

  • CAS Number: 94061-81-1
  • MF: C24H25FNNaO4
  • MW: 434.45600
  • Catalog: HMG-CoA Reductase (HMGCR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A