Rosuvastatin Calcium - CAS 147098-20-2
Catalog number: B0084-084352
Category: Inhibitor
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HMG-CoA Reductase (HMGCR)
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
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B0084-084352 2 g $199 In stock
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ZD4522; ZD 4522; ZD-4522
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1.Development of a Stability-Indicating Stereoselective Method for Quantification of the Enantiomer in the Drug Substance and Pharmaceutical Dosage Form of Rosuvastatin Calcium by an Enhanced Approach
Rajendra Reddy G1, Ravindra Reddy P1, Siva Jyothi P1. Sci Pharm. 2014 Dec 5;83(2):279-96. doi: 10.3797/scipharm.1410-09. eCollection 2015.
A novel, simple, precise, and stability-indicating stereoselective method was developed and validated for the accurate quantification of the enantiomer in the drug substance and pharmaceutical dosage forms of Rosuvastatin Calcium. The method is capable of quantifying the enantiomer in the presence of other related substances. The chromatographic separation was achieved with an immobilized cellulose stationary phase (Chiralpak IB) 250 mm x 4.6 mm x 5.0 μm particle size column with a mobile phase containing a mixture of n-hexane, dichloromethane, 2-propanol, and trifluoroacetic acid in the ratio 82:10:8:0.2 (v/v/v/v). The eluted compounds were monitored at 243 nm and the run time was 18 min. Multivariate analysis and statistical tools were used to develop this highly robust method in a short span of time. The stability-indicating power of the method was established by subjecting Rosuvastatin Calcium to the stress conditions (forced degradation) of acid, base, oxidative, thermal, humidity, and photolytic degradation.
2.Risks of Adverse Events Following Coprescription of Statins and Calcium Channel Blockers: A Nationwide Population-Based Study.
Wang YC1, Hsieh TC, Chou CL, Wu JL, Fang TC. Medicine (Baltimore). 2016 Jan;95(2):e2487. doi: 10.1097/MD.0000000000002487.
Some statins (simvastatin, lovastatin, and atorvastatin) are metabolized by cytochrome P450s 3A4 (CYP3A4). Inhibitors of CYP3A4 including some calcium channel blockers (CCBs) might increase statin blood concentration, owing to drug-drug interactions. Risk of adverse events such as acute kidney injury might occur following the coprescription of CYP3A4-metabolized statins and CCBs that inhibit CYP3A4.This was a population-based cohort study. The study analyzed data of patients treated between 1997 and 2011, retrieved from Taiwan's National Health Insurance database. We enrolled 32,801 patients who received coprescription of statins and CCBs that inhibit CYP3A4 (amlodipine, diltiazem, felodipine nicardipine, nifedipine, and verapamil). These patients were divided into 2 groups, according to whether they had received CYP3A4-metabolized statins (lovastatin, simvastatin, and atorvastatin) or non-CYP3A4-metabolized statins (fluvastatin, rosuvastatin, and pitavastatin).
Herbet M, Gawrońska-Grzywacz M, Jagiełło-Wójtowicz E. Acta Pol Pharm. 2015 Mar-Apr;72(2):261-5.
The aim of this study was to assess the effect of a combined 14-day treatment with rosuvastatin (10 mg/kg) and fluoxetine (10 mg/kg) on selected biochemical parameters of oxidative stress in the blood of rats. The activity of glutathione peroxidase (GPX), glutathione reductase (GR) and the total antioxidant status (TAS) were determined. A combined 14-day treatment with rosuvastatin and fluoxetine significantly increases glutathione peroxidase and glutathione reductase activity and decreases the level of TAS. Rosuvastatin administered to rats caused a decrease in the glutathione peroxidase activity and an increase in the glutathione reductase activity but did not affect the level of TAS. A 14-day treatment with fluoxetine exerted practically no effect on the investigated parameters of oxidative stress in rats. The abovementioned changes in the biochemical parameters after the combined treatment with rosuvastatin and fluoxetine may imply an imbalance in prooxidant and antioxidant levels in the combined treatment with rosuvastatin and fluoxetine.
4.[The interactions between natural products and OATP1B1].
Shi MZ, Liu Y, Bian JL, Jin M, Gui CS. Yao Xue Xue Bao. 2015 Jul;50(7):848-53.
Organic anion transporting polypeptide 1B1 (OATP1B1) is an important liver-specific uptake transporter, which mediates transport of numerous endogenous substances and drugs from blood into hepatocytes. To identify and investigate potential modulators of OATP1B1 from natural products, the effect of 21 frequently used natural compounds and extracts on OATP1B1-mediated fluorescein methotrexate transport was studied by using Chinese hamster ovary cells stably expressing OATP1B1 (CHO-OATP1B1) in 96-well plates. This method could be used for the screening of large compound libraries. Our studies showed that some flavonoids (e.g., quercetin, quercitrin, rutin, chrysanthemum flavonoids and mulberrin) and triterpenoids (e.g., glycyrrhetinic acid and glycyrrhizic acid) were inhibitors of OATP1B1 with IC50 values less than 16 µmol · L(-1). The IC50 value of glycyrrhetinic acid on OATP1B1 was comparable to its blood concentration in clinics, indicating an OATPlB1-mediated drug-drug interaction could occur.
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CAS 147098-20-2 Rosuvastatin Calcium

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