| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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| 50g |
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| Other Sizes |
| Targets |
Rosuvastatin targets HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol synthesis. By inhibiting this enzyme, it reduces the production of cholesterol in the liver. It also has an IC50 of 11 nM for HMGCR and potently blocks the hERG potassium channel with an IC50 of 195 nM.
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| ln Vitro |
In vitro, rosuvastatin inhibits HMG-CoA reductase with an IC50 of 5 nM and inhibits cholesterol synthesis in isolated rat hepatocytes with an IC50 of 0.16 nM. It is a competitive inhibitor of HMGCR. These studies demonstrate its high potency in reducing cholesterol synthesis at the cellular level.
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| ln Vivo |
Rosuvastatin sodium (10 mg/kg, i.p.) prolongs the QTc from 201±1 msec to 210±2 msec in awake and unrestrained guinea pigs [2]. Rosuvastatin (20 mg/kg/day for 2 weeks) significantly lowers very low-density lipoprotein sodium (VLDL) in streptozotocin-induced diabetic rats [4].
In vivo, rosuvastatin is an effective lipid-lowering agent. It is administered orally and significantly reduces LDL-C levels in patients with hyperlipidemia. It has been shown to decrease plasma cholesterol levels in animal models fed a high-fat diet. Its clinical efficacy is well-established in numerous large-scale trials. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for rosuvastatin measures its ability to inhibit HMG-CoA reductase activity. The assay is performed using purified HMGCR enzyme and radiolabeled HMG-CoA as a substrate. The conversion of HMG-CoA to mevalonate is measured, and the IC50 is calculated. This is the primary assay for determining its potency as a statin.
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| Cell Assay |
In vitro cellular studies are conducted using hepatocytes, such as primary rat hepatocytes or human HepG2 cells. Cells are treated with rosuvastatin, and cholesterol synthesis is measured by monitoring the incorporation of radiolabeled acetate or other precursors into cholesterol. The IC50 for cholesterol synthesis inhibition is determined.
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| Animal Protocol |
In vivo animal experiments are performed in animal models of hyperlipidemia, such as rats or hamsters fed a high-cholesterol diet. Rosuvastatin is administered orally for a defined period. Blood samples are collected to measure plasma lipid levels (total cholesterol, LDL-C, HDL-C, triglycerides), and the liver is harvested to assess HMGCR activity and cholesterol content.
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| ADME/Pharmacokinetics |
Rosuvastatin Sodium has a molecular formula of C22H27FN3NaO6S and a molecular weight of 503.52 g/mol. It is a white to off-white crystalline solid. It is soluble in DMSO and PBS (pH 7.2). For research, it is typically stored at -20°C. It is an oral drug with good bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for rosuvastatin are well-documented from its clinical use. It is generally well-tolerated, but like all statins, it can cause myopathy, liver enzyme elevations, and, rarely, rhabdomyolysis. It is contraindicated in pregnancy and in patients with active liver disease. Its safety profile is established for therapeutic use.
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| References | |
| Additional Infomation |
Rosuvastatin Sodium is marketed under the brand name Crestor and is one of the most potent statins available. It is also known as ZD 4522. It is used to treat hyperlipidemia and to reduce the risk of cardiovascular events. It is a competitive inhibitor of HMG-CoA reductase and is a widely prescribed medication.
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| Molecular Formula |
C22H27FN3O6S.NA.
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|---|---|
| Molecular Weight |
503.5
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| Exact Mass |
503.15
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| CAS # |
147098-18-8
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| Related CAS # |
Rosuvastatin Calcium;147098-20-2;Rosuvastatin-d3 sodium;1279031-70-7;Rosuvastatin;287714-41-4;Rosuvastatin-d6 sodium;2070009-41-3;Rosuvastatin-d6 calcium
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| PubChem CID |
23684378
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| Appearance |
White to light yellow solid powder
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| Melting Point |
128-131℃
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| LogP |
2.147
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
773
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)C1=NC(=NC(=C1/C=C/[C@H](C[C@H](CC(=O)[O-])O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C.[Na+]
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| InChi Key |
RGEBGDYYHAFODH-DHMAKVBVSA-M
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| InChi Code |
InChI=1S/C22H28FN3O6S.Na/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32;/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30);/q;+1/p-1/b10-9+;/t16-,17-;/m1./s1
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| Chemical Name |
sodium;(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate
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| Synonyms |
Rosuvastatin Sodium; S4522; ZD-4522; trade name: Crestor
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~496.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9861 mL | 9.9305 mL | 19.8610 mL | |
| 5 mM | 0.3972 mL | 1.9861 mL | 3.9722 mL | |
| 10 mM | 0.1986 mL | 0.9930 mL | 1.9861 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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