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6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-

Base Information Edit
  • Chemical Name:6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-
  • CAS No.:147098-20-2
  • Molecular Formula:2(C22H27FN3O6S).Ca
  • Molecular Weight:1001.14
  • Hs Code.:29350090
  • European Community (EC) Number:627-028-1
  • Mol file:147098-20-2.mol
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-

Synonyms:6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-;147098-20-2;SCHEMBL153040;SCHEMBL153041

Suppliers and Price of 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-
Supply Marketing:Edit
Business phase:
The product has achieved commercial mass production*data from LookChem market partment
Manufacturers and distributors:
  • Manufacture/Brand
  • Chemicals and raw materials
  • Packaging
  • price
  • TRC
  • RosuvastatinCalciumSalt
  • 50mg
  • $ 55.00
  • Tocris
  • Rosuvastatin Calcium ≥99%(HPLC)
  • 10
  • $ 75.00
  • Tocris
  • Rosuvastatin Calcium ≥99%(HPLC)
  • 50
  • $ 317.00
  • TCI Chemical
  • Rosuvastatin Calcium >95.0%(HPLC)(N)
  • 200mg
  • $ 154.00
  • Medical Isotopes, Inc.
  • RosuvastatinCalciumSalt
  • 100 mg
  • $ 290.00
  • DC Chemicals
  • Rosuvastatin Calcium >99%
  • 1 g
  • $ 1200.00
  • DC Chemicals
  • Rosuvastatin Calcium >99%
  • 100 mg
  • $ 300.00
  • CSNpharm
  • Rosuvastatin Calcium
  • 5mg
  • $ 43.00
  • CSNpharm
  • Rosuvastatin Calcium
  • 100mg
  • $ 92.00
  • ChemScene
  • Rosuvastatin Calcium 99.94%
  • 10mg
  • $ 60.00
Total 274 raw suppliers
Chemical Property of 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)- Edit
Chemical Property:
  • Appearance/Colour:white to off-white crystalline solid 
  • Melting Point:122 °C 
  • Boiling Point:745.6 °C at 760 mmHg 
  • Flash Point:404.7 °C 
  • PSA:304.26000 
  • Density:== 
  • LogP:4.29560 
  • Storage Temp.:-20°C Freezer 
  • Hydrogen Bond Donor Count:3
  • Hydrogen Bond Acceptor Count:10
  • Rotatable Bond Count:10
  • Exact Mass:521.1308758
  • Heavy Atom Count:34
  • Complexity:767
Purity/Quality:

≥98.0% *data from raw suppliers

RosuvastatinCalciumSalt *data from reagent suppliers

Safty Information:
  • Pictogram(s):  
  • Hazard Codes: 
MSDS Files:

SDS file from LookChem

Useful:
  • 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.[Ca]
  • Isomeric 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.[Ca]
  • Recent EU Clinical Trials:An Open-Label Long-Term Extension to the Randomized, Double-blind, Placebo-controlled, Multi-center, Cross-over Study of Rosuvastatin in Children and Adolescents (aged 6 to <18 years) with Homozygous Familial Hypercholesterolemia (HoFH)
  • Drug Interactions 1. Cyclosporine: when this product is used in combination with cyclosporine, the AUC of rosuvastatin is averagely 7 times higher than that observed in healthy volunteers (compared with the same dose using this service). Combination usage does not affect the plasma concentrations of cyclosporine. 2. Vitamin K antagonists: same as other HMG-CoA reductase inhibitor, for patients of simultaneously usage of vitamin K antagonists (such as warfarin), at the beginning or gradually increasing the dose of this product may cause the increase of INR (international normalized ratio). Stop using the product or gradually decreasing the dose can lead to decrease in INR. In this case, appropriate INR testing is needed. 3. Combination of gemfibrozil, fenofibrate, other fibrates and lipid-lowering doses (≥1g/day) of niacin with HMG-CoA reductase inhibitors can increase the risk of myopathy, which may be due to that they can cause myopathy when given alone. 4. Antacids: Mixing the product and one antacid containing aluminum hydroxide and magnesium for suspension can reduce the concentration of statin rosuvastatin plasma by 50%. Taking antacids two hours after taking this can further reduce the impact. The clinical significance of this drug interaction has not been studied. 5. Erythromycin: Combination with erythromycin can cause rosuvastatin AUC (0~t) decrease by 20% and Cmax decrease by 30%. This interaction may be due to the gastrointestinal motility caused by increase of erythromycin. 6. Oral administration of contraceptives/hormone replacement therapy (HRT): while using this drug together with oral contraceptives can cause the increase of ethinyl estradiol and norgestrel AUC by 26% and 34%, respectively. When choosing the dose of oral contraceptives, the patients should consider the increase of the plasma concentration of these drugs. Yet there are no pharmacokinetic data on taking rosuvastatin and HRT together. Therefore, we cannot exclude the presence of similar interactions. However, in clinical trials, this kind of combination is widely applied and can be well tolerated by patients.
  • Indications Primary Hypercholesterolemia: Usual dose of rosuvastatin calcium (10 mg) can significantly reduce LDLC levels in patients of primary hypercholesterolemia, and has a better efficacy compared with atorvastatin calcium (10mg). At the end of the experiment, TC, TG levels drop even more. Moreover, 5 mg of rosuvastatin calcium within the same eight weeks of treatment has a better effect on reducing LDLC level compared with 10 mg atorvastatin calcium. The difference is statistically significant, suggesting that the lipid-lowering effect of rosuvastatin calcium is better than that of atorvastatin calcium. Our experimental results are also consistent with the other previous assessment (STELLAR, MERCURY) about efficacy studies on statin drugs. Rosuvastatin calcium has a stronger LDLC-lowering effect than the other statins drugs (atorvastatin, simvastatin and pravastatin), allowing more patients to achieve recommended treatment goals. Elderly coronary heart disease combined hyperlipidemia: Rosuvastatin calcium is capable of competitively inhibiting liver methylglutaryl coenzyme A reductase, and further exerts its good effect on reducing the fat. It has a long half-life. The gender and age of patients have no significant effect on the metabolism of drugs. The drug has only a few of adverse reactions. Meanwhile, the drug can also effectively promote the transport of low-density lipoprotein into cells, thus improving the cleaning effect of LDL, and playing a role in effectively lowering LDL. In addition, rosuvastatin calcium may also inhibit the aggregation of platelet, reduce the body's inflammatory response and protect their endothelial cells, effectively stabilize the plaque of patients suffering coronary artery disease to reduce its impact on the patient. The patients of experimental group in our hospital were treated with rosuvastatin calcium, which gives a significantly better lipid-lowering effect than patients in the control group, P <0.05, the difference was statistically significant. This further illustrates the usage of rosuvastatin calcium for treatment of elderly coronary heart disease combined hyperlipidemia has a good effect which can improve efficacy, reduce the blood fat with high clinical significance.
  • Uses For making lipid-lowering drugs. Rosuvastatin Calcium Salt is a selective, competitive HMG-CoA reductase inhibitor. Antilipemic. A selective, competitive HMG-CoA reductase inhibitor. Antilipemic. antiinflammatory, glucocorticoid antirheumatic
  • Description Rosuvastatin, one of the two new statins launched for the treatment of hypercholesterolemia, has high hepato-selectivity and more potent inhibitory effect on HMG-CoA reductase than the previously marketed statins. In rat hepatocytes, it inhibits cholesterol biosynthesis with an IC50 of 1.12 nM, which is ~100-fold higher potency than pravastatin. Rosuvastatin is synthesized in a 12-step sequence, entailing the construction of a pyrimidinyl aldehyde intermediate in eight steps and subsequent introduction of the dihydroxyheptenoate side chain via Wittig reaction with a bketophosphorane reagent and stereoselective carbonyl reduction of the resultant enone. Pharmacokinetic properties of rosuvastatin in humans, dosed at 5–80 mg, are approximately linear with dose. Following oral administration, rosuvastatin is rapidly absorbed with an oral bioavailability of ~20% and tmax of ~3 h. It has a prolonged duration of action, with terminal t1/2 of ~20 h, compatible with once-daily dosing. In humans, rosuvastatin is minimally metabolized through CYP2C9 and CYP2C19, with little or no metabolism via the CYP3A4. Approximately 90% of the administered oral dose is eliminated in the feces (92% as the parent compound) and the rest in the urine. Rosuvastatin is considered a “superstatin” due to its ability, at well-tolerated doses, to lower LDL cholesterol and triglycerides to a much greater extent than first generation statins. In patients with hypercholesterolemia, rosuvastatin treatment at doses of 5 and 10 mg/day over 12-week period resulted in 40–43% reduction of LDL-cholesterol levels, 12–13% increase in HDL-cholesterol, and 17– 19% reduction in triglycerides. In comparison, the efficacy range of LDL-cholesterol reductions by atorvastatin (10 mg/day), pravastatin (20 mg/day), and simvastatin (20 mg/day) was 28–35%. Rosuvastatin is a well-tolerated drug at doses of 1–20 mg and the most common side effects at these doses are headache, myalgia, pain and pharyngitis, which are consistent with those previously reported for statin therapy.
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