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| 2g |
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| 5g |
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Rosuvastatin sodium (formerly S4522; ZD-4522, trade name: Crestor), the sodium salt of Rosuvastatin, is an HMG-CoA reductase inhibitor approved for the treatment of high cholesterol and related conditions such as dyslipidemia, and to prevent cardiovascular disease. It inhibits HMG-CoA reductase with an IC50 of 11 nM in a cell-free assay. Rosuvastatin belongs to the statin class of antihyperliperdemic drugs.
| 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].
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| References |
| Molecular Formula |
C22H27FN3O6S.NA.
|
|---|---|
| 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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