Rosuvastatin
Rosuvastatin (CAS 287714-41-4) is a small molecule that acts as a competitive inhibitor of the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, a critical enzyme catalyzing the rate-limiting step in cholesterol biosynthesis. The compound exhibits potent inhibitory activity, demonstrated by an IC50 value of approximately 11 nM. By inhibiting HMG-CoA reductase, rosuvastatin effectively reduces the biosynthesis of cholesterol, facilitating its application in research focused on lipid metabolism, cardiovascular diseases, and related cellular pathways.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 481.54 |
| Cas No. | 287714-41-4 |
| Formula | C22H28FN3O6S |
| Solubility | ≥48.2 mg/mL in DMSO; ≥10.78 mg/mL in H2O with ultrasonic; ≥12.4 mg/mL in EtOH with ultrasonic |
| Chemical Name | (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(C)C1=NC(=NC(=C1C=CC(CC(CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Rat isolated hepatocytes |
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Reaction Conditions |
1.12 nM (IC50) |
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Applications |
Rosuvastatin inhibited the incorporation of sodium [14C]acetate into cholesterol with an IC50 value of 1.12 nM, and its inhibitory activity on cholesterol biosynthesis was approximately 100 times more potent than pravastatin. |
| Animal experiment:[1] | |
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Animal models |
Normolipemic male beagle dogs |
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Dosage form |
3 mg/kg/day Administered orally for 14 days |
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Applications |
In male beagle dogs with normal cholesterol levels, rosuvastatin (3 mg/kg/day) administration for 14 days decreased plasma cholesterol levels by 26%, higher than 18% in the pravastatin treatment group. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Watanabe M, Koike H, Ishiba T, et al. Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorganic & Medicinal Chemistry, 1997, 5(2): 437-444. |
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Quality Control & MSDS
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Chemical structure
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