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Research for Hypercholesterolemia
HMG-CoA Reductase Inhibitors

Competitive inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase are the rate limiting enzymes in cholesterol biosynthesis. By blocking the conversion of HMG-CoA to the cholesterol precursor mevalonate, these agents inhibit hepatic synthesis of cholesterol, causing a subsequent stimulation of LDL receptors and an increase in the clearance of LDL and its precursor particles from the circulation.



  INDEX
  1. Rosuvastatin Calcium Salt   NEW


  1. Atorvastatin Calcium Trihydrate
  2. Compactin [Mevastatin]
  3. Fluvastatin Sodium
  4. Lovastatin
  5. Pitavastatin Calcium
  6. Pravastatin Sodium Salt
  7. Simvastatin

  1. Reference
  2. Product List



1. Rosuvastatin Calcium Salt - NEW -
The inhibitory activity is stronger than that of other HMG-CoA Reductase inhibitors.
  • Appearance: white - slightly pale brown, crystals - powder
  • Solubility in methanol: to pass test
  • Assay (HPLC): 90+ % (The first lot: 99.3%)
  • IC50=12 nmol/L 1)
  • CAS No.: 147098-20-2
  • C22H27FN3O6S)2·Ca = 1001.14
Compactin



2. Atorvastatin Calcium Trihydrate
This drug is almost comparable to simvastatin and shows inhibitory activity about 5 times that of pravastatin sodium.
  • Appearance: white - slightly pale brown, crystals - powder
  • Solubility in dimethylsulfoxide: to pass test
  • Assay (HPLC): 98.0 %
  • IC50=1.9 μmol/L 1)
  • CAS No.: 134523-03-8
  • C66H68CaF2N4O4O10·3H2O = 1209.39
Compactin


3. Compactin [ Mevastatin ]
This is a HMG-CoA reductase inhibitor discovered from Penicillium citrinum, a strain of blue molds. It induces reversible G1 arrest. It also inhibits farnesylation of Ras protein, which is a product of ras gene known as a carcinogenic gene.
  • Appearance: white - nearly white, crystalline powder - powder
  • Solubility in ethanol: to pass test
  • Assay (HPLC): 95.0 %
  • IC50=1.29 μmol/L 1)
  • CAS No.: 73573-88-3
  • C23H34O5 = 390.51
Compactin
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4. Fluvastatin Sodium
It is a synthetic HMG-CoA reductase inhibitor. It exhibits antioxidant action.
  • Appearance: white - pale brown, crystalline powder - powder
  • Solubility in methanol: to pass test
  • Assay (HPLC): min. 98.0 %
  • IC50=7.4 nmol/l1)
  • CAS No.: 93957-55-2
  • C24H25FNNaO4=433.45
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5. Lovastatin
This is a HMG-CoA reductase inhibitor discovered from Aspergillus terreus, a strain of aspergillus. It is an analog of compactin. It is useful in cancer research as it inhibits farnesylation of Ras protein, which is a product of ras gene known as a carcinogenic gene. .
  • Appearance: white - nearly white, crystals - powder or mass
  • Solubility in ethanol: to pass test
  • Assay (HPLC): 95.0 %
  • IC50=0.58 μmol/L 1)
  • CAS No.: 75330-75-5
  • C24H36O5 = 404.54
Lovastatin


6. Pitavastatin Calcium
This is a HMG-CoA reductase inhibitor more potent than simvastatin or pravastatin.
  • Appearance: white - slightly pale yellow, crystalline powder - powder
  • Solubility in dil.HCl: to pass test
  • Assay (HPLC): more than 98.0 %
  • IC50=6.8nmol/l2)
  • CAS No.: 147526-32-7
  • C50H46CaF2N2O8 = 880.98
Pitavastatin
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7. Pravatatin Sodium Salt
This is a derivative with a structure similar to lovastatin. It is useful in cancer research as it inhibits farnesylation of Ras protein, which is a product of ras gene known as a carcinogenic gene. It is a sodium salt and, therefore, freely soluble in water.
  • Appearance: white - pale yellow, crystals - powder
  • Solubility in acetonitrile: to pass test
  • Assat (HPLC): more than 98.0 %
  • IC50=46 nmol/l2)
  • CAS No.: 81131-70-6
  • C23H35NaO7=446.51

Pravastatin



8. Simvastatin
This is a derivative with a structure similar to lovastatin. It exhibits inhibitory action about 3 times that of pravastatin. It is useful in cancer research as it inhibits farnesylation of Ras protein, which is a product of ras gene known as a carcinogenic gene. It is a sodium salt and, therefore, freely soluble in water.
  • Appearance: white - nearly white, crystals - powder
  • Solublity in acetonitrile: to pass etSolubility in acetonitrile: to pass test/li>
  • Assay (HPLC): 98.0 %
  • IC50=16 nmol/l 2)
  • CAS No.: 79902-63-9
  • C25H38O5 = 418.57
Simvastatin


9. Reference
10. Product List
Description Package Size Wako Catalog No.
Atorvastatin Calcium Trihydrate 10 mg
50 mg
500 mg
012-23901
018-23903
016-23904
Compactin [Mevastatin] 25 mg 033-17301
Fluvastatin Sodium 50 mg
500 mg
069-05571
065-05573
Lovastatin 25 mg 125-04581
Pitavastatin Calcium 10 mg
100 mg
163-24861
169-24863
Pravastatin Sodium Salt 25 mg
100 mg
162-19821
168-19823
Rosuvastatin Calcium Salt   - NEW - 50 mg
250 mg
186-02731
182-02733
Simvastatin 25 mg
100 mg
193-12051
199-12053
QUOTATION REQUEST for HMG-CoA Reductase Inhibitors

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