| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Rosuvastatin Calcium (S-4522, Rosuvastatin hemicalcium; ZD-4522; ZD4522, trade name: Crestor), a member of the statin class of lipid-lowering drugs, is a potent and competitive inhibitor of HMG-CoA reductase with potential anti-hyperlipidemic activity. It inhibits HMG-CoA reductase with an IC50 of 11 nM in a cell-free assay. Rosuvastatin belongs to the statin class that hasd been approved for use in the treatment of high cholesterol and related conditions such as dyslipidemia, and to prevent cardiovascular disease. Its approximate elimination half life is 19 h and its time to peak plasma concentration is reached in 3–5 h following oral administration. In 2013 Crestor was the fourth-highest selling drug in the United States, accounting for approx. $5.2 billion in sales.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
In awake and unrestrained guinea pigs, rosuvastatin calcium (10 mg/kg, intraperitoneal) prolongs QTc from 201±1 to 210±2 ms[2]. In diabetic mellitus rats generated by streptozocin, rosuvastatin (20 mg/kg/day) for two weeks significantly lowers very low-density lipoproteins (VLDL)[4].
|
||
| Animal Protocol |
|
||
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Levels of rosuvastatin in milk are low, but no relevant published information exists with its use during breastfeeding. The consensus opinion is that women taking a statin should not breastfeed because of a concern with disruption of infant lipid metabolism. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk A possible case of rosuvastatin-induced gynecomastia has been reported. Serum prolactin was not measured. |
||
| References |
[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44.
[2]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7. [3]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78. [4]. Feng PF, et al. Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane. Mol Pharm. 2019 Apr 1;16(4):1477-1488. |
||
| Additional Infomation |
Rosuvastatin calcium is an organic calcium salt that is the hemicalcium salt of rosuvastatin. It has a role as an anti-inflammatory agent, a CETP inhibitor and a cardioprotective agent. It is an organic calcium salt and a N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine. It contains a rosuvastatin(1-).
Rosuvastatin Calcium is the calcium salt form of rosuvastatin, a statin with antilipidemic activity. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. A HYDROXYMETHYLGLUTARYL-COA-REDUCTASE INHIBITOR, or statin, that reduces the plasma concentrations of LDL-CHOLESTEROL; APOLIPOPROTEIN B, and TRIGLYCERIDES while increasing HDL-CHOLESTEROL levels in patients with HYPERCHOLESTEROLEMIA and those at risk for CARDIOVASCULAR DISEASES. See also: Rosuvastatin (has active moiety); Ezetimibe; rosuvastatin calcium (component of). Drug Indication Homozygous Familial Hypercholesterolaemia, Prevention of cardiovascular events, Primary combined (mixed) dyslipidaemia, Primary hypercholesterolaemia |
| Molecular Formula |
C22H28FN3O6S.1/2CA
|
|---|---|
| Molecular Weight |
500.57
|
| Exact Mass |
1000.283
|
| CAS # |
147098-20-2
|
| Related CAS # |
Rosuvastatin Sodium;147098-18-8;Rosuvastatin-d3 sodium;1279031-70-7;Rosuvastatin Calcium (Standard);147098-20-2;Rosuvastatin;287714-41-4;Rosuvastatin-d3;1133429-16-9;Rosuvastatin-d6 sodium;2070009-41-3;Rosuvastatin-d6 calcium
|
| PubChem CID |
5282455
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
745.6ºC at 760 mmHg
|
| Melting Point |
122ºC
|
| Flash Point |
404.7ºC
|
| LogP |
4.295
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
67
|
| Complexity |
761
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2]
|
| InChi Key |
LALFOYNTGMUKGG-BGRFNVSISA-L
|
| InChi Code |
InChI=1S/2C22H28FN3O6S.Ca/c2*1-13(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;/h2*5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30);/q;;+2/p-2/b2*10-9+;/t2*16-,17-;/m11./s1
|
| Chemical Name |
calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate
|
| Synonyms |
ZD 4522; Rosuvastatin calcium; S-4522; Rosuvastatin hemicalcium; ZD-4522; ZD4522; S 4522; S4522; ZD 4522 calcium salt; ZD 4522 Calcium; Brand name: Crestor.
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.16 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 (4.16 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 (4.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+30% PEG 300+dd H2O:10 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9977 mL | 9.9886 mL | 19.9772 mL | |
| 5 mM | 0.3995 mL | 1.9977 mL | 3.9954 mL | |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9977 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03216304 | Completed | Drug: 20 mg rosuvastatin calcium period 2 |
Healthy | Cross Research S.A. | May 22, 2017 | Phase 1 |
| NCT02569645 | Completed | Drug: Rosuvastatin | Rectal Cancer | AHS Cancer Control Alberta | November 2015 | Phase 2 |
| NCT01524601 | Completed | Drug: Rosuvastatin | Disorder Related to Renal Transplantation |
University of Oslo School of Pharmacy | February 2012 | Phase 4 |
| NCT04846231 | Completed Has Results | Drug: Rosuvastatin Other: Placebo |
Hypercholesterolemia | The Cleveland Clinic | April 23, 2021 | Phase 2 |
Effect of rosuvastatin on thrombin-stimulated leukocyte rolling (upper panel) and leukocyte adherence (lower panel) in rat mesenteric venules.Br J Pharmacol.2001 Jun;133(3):406-12. |
|---|
Mevalonic acid blocks the inhibitory effect of rosuvastatin on thrombin-stimulated leukocyte rolling (upper panel) and leukocyte adherence (lower panel).Br J Pharmacol.2001 Jun;133(3):406-12. |
Leukocyte rolling (upper panel) and leukocyte adherence (lower panel) in peri-intestinal venules of wild-type mice, eNOS−/−mice, and eNOS−/−mice given 1.25 mg kg−1rosuvastatin.Br J Pharmacol.2001 Jun;133(3):406-12. |
Immunohistochemical analysis of P-selectin expression on rat ileal venules, expressed as percentage of venules staining positive for P-selectin.Br J Pharmacol.2001 Jun;133(3):406-12. |
|---|
Effect of rosuvastatin on NO release in rat aortic segments. Basal release of nitric oxide is expressed as nanomoles per mg tissue.Br J Pharmacol.2001 Jun;133(3):406-12. |
Effect of rosuvastatin on thrombin-stimulated leukocyte extravasation. Rat mesenteries were superfused with either K-H buffer alone or with 0.5 u ml−1thrombin. Rosuvastatin (1.25 mg kg−1) was administered intraperitoneally 18 h prior to the study.Br J Pharmacol.2001 Jun;133(3):406-12. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
