RosuvastatinCAS# 287714-41-4 |
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Quality Control & MSDS
3D structure
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| Cas No. | 287714-41-4 | SDF | Download SDF |
| PubChem ID | 6439133 | Appearance | Powder |
| Formula | C22H28FN3O6S | M.Wt | 481.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ZD 4522 | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | (E,3R,5R)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid | ||
| 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 | ||
| Standard InChIKey | BPRHUIZQVSMCRT-YXWZHEERSA-N | ||
| Standard InChI | InChI=1S/C22H28FN3O6S/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)/b10-9+/t16-,17+/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
IC50 Value: 11 nM [1]
Target: HMG-CoA reductase
in vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].
in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5]. References: | |||||
Rosuvastatin Dilution Calculator
Rosuvastatin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0767 mL | 10.3834 mL | 20.7667 mL | 41.5334 mL | 51.9168 mL |
| 5 mM | 0.4153 mL | 2.0767 mL | 4.1533 mL | 8.3067 mL | 10.3834 mL |
| 10 mM | 0.2077 mL | 1.0383 mL | 2.0767 mL | 4.1533 mL | 5.1917 mL |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 0.8307 mL | 1.0383 mL |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.4153 mL | 0.5192 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
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A randomized, controlled comparison of different intensive lipid-lowering therapies in Chinese patients with non-ST-elevation acute coronary syndrome (NSTE-ACS): Ezetimibe and rosuvastatin versus high-dose rosuvastatin.[Pubmed:28291622]
Int J Cardiol. 2017 May 15;235:49-55.
BACKGROUND: Statin combined with ezetimibe demonstrates significant benefit in lowering low density lipid cholesterol (LDL-C) and cardiovascular events abroad, but whether intermediate intensity statins combined with ezetimibe is superior to high-intensity statin monotherapy in Chinese people is unknown. METHODS: A total of 125 patients were randomly assigned to a intermediate intensity Rosuvastatin group (Rosuvastatin 10mg/d, n=42), high-dose Rosuvastatin group (Rosuvastatin 20mg/d, n=41) or combination therapy group (ezetimibe 10mg/d and Rosuvastatin 10mg/d, n=42) with a 12-week follow-up. The primary end point was the proportion of patients who achieved the 2011 ESC/EAS LDL-C goal <70mg/dL (1.8mmol/L) at week 12. Secondary end points included changes from baseline in lipids, the occurrence of all cardiovascular events, high-sensitivity C-reactive protein and safety markers. RESULTS: The combination therapy group in the primary end point was significantly higher than Rosuvastatin (20mg) and Rosuvastatin (10mg) at week 12 (81.0% vs 68.3% vs 33.3%, P<0.001). And the similar change was observed in reducing LDL-C levels at week 12 (67.28% vs 52.80% vs 43.89%, P<0.001). The incidence of drug-related adverse events was much higher in the Rosuvastatin 20mg group than the Rosuvastatin 10mg group and the combination therapy group (17.0% vs 2.4% vs 4.8%, P<0.05). CONCLUSIONS: The combination of Rosuvastatin 10mg/ezetimibe 10mg was an effectively alternative therapy superior to Rosuvastatin 20mg or 10mg with a greater effect on lowering LDL-C and a lower incidence of drug-related adverse events in Chinese patients.
[Rosuvastatin in Coronary Bypass Surgery: Whether Only Secondary Prevention?][Pubmed:28294868]
Kardiologiia. 2016 May;56(5):18-23.
BACKGROUND AND AIM: The increasing number of coronary artery bypass grafting (CABG) is associated with a need for active introduction of methods improving immediate and long-term results of these interventions. Results of a number of studies conducted during recent years allow to consider high dose statin therapy one of such methods. In this article we present results of Rosuvastatin administration to patients with ischemic heart disease (IHD) prior to surgery. METHODS: Rosuvastatin (40 mg/day) was given for 4 weeks before CABG to patients who had previously taken simvastatin (20 mg/day). RESULTS: This regimen was assocaed with reduction of desquamation of endothelium of the intima, reduction of the number of smooth muscle cells in the media, as well as the proliferation index according to the immunohistochemical analysis in sections of the great saphenous vein selected for the coronary anastomosis. CONCLUSION: It is assumed that the antiproliferative effects of high-dose Rosuvastatin therapy may have a positive impact in relation to the viability of a remote arterio-venous grafts.
Investigating Transporter-Mediated Drug-Drug Interactions Using a Physiologically Based Pharmacokinetic Model of Rosuvastatin.[Pubmed:28296193]
CPT Pharmacometrics Syst Pharmacol. 2017 Apr;6(4):228-238.
Rosuvastatin is a frequently used probe in transporter-mediated drug-drug interaction (DDI) studies. This report describes the development of a physiologically based pharmacokinetic (PBPK) model of Rosuvastatin for prediction of pharmacokinetic (PK) DDIs. The Rosuvastatin model predicted the observed single (i.v. and oral) and multiple dose PK profiles, as well as the impact of coadministration with transporter inhibitors. The predicted effects of rifampin and cyclosporine (6.58-fold and 5.07-fold increase in Rosuvastatin area under the curve (AUC), respectively) were mediated primarily via inhibition of hepatic organic anion-transporting polypeptide (OATP)1B1 (Inhibition constant (Ki ) approximately 1.1 and 0.014 microM, respectively) and OATP1B3 (Ki approximately 0.3 and 0.007 microM, respectively), with cyclosporine also inhibiting intestinal breast cancer resistance protein (BCRP; Ki approximately 0.07 microM). The predicted effects of gemfibrozil and its metabolite were moderate (1.88-fold increase in Rosuvastatin AUC) and mediated primarily via inhibition of hepatic OATP1B1 and renal organic cation transporter 3. This model of Rosuvastatin will be useful in prospectively predicting transporter-mediated DDIs with novel pharmaceutical agents in development.
