Rosuvastatin (ZD4522) calcium

For research use only.

Catalog No.S2169

8 publications

Rosuvastatin (ZD4522) calcium Chemical Structure

CAS No. 147098-20-2

Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.

Selleck's Rosuvastatin (ZD4522) calcium has been cited by 8 publications

1 Customer Review

  • MDA-MB-231 cells were treated with simvastatin (SIM) or rosuvastatin (ROSU) in combination with ZOL for 48 h. Vitality and apoptosis were measured by using the cell titer blue and the caspase 3/7 Glo assay. Data are shown as mean ± SD of at least three individual experiments (*p ≤ 0.05; **p ≤ 0.01; ***p ≤ 0.001).

    Cancer Lett, 2016, 375(1):162-71. . Rosuvastatin (ZD4522) calcium purchased from Selleck.

Purity & Quality Control

Choose Selective HMG-CoA Reductase Inhibitors

Biological Activity

Description Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
Targets
HMG-CoA reductase [2]
(Cell-free assay)
11 nM
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. [1] 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. [2] 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 is efficient on reducing plasma liquids. 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% [2] 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] Rosuvastatin (20 mg/kg) inhibits ROS production, normalizes NO-dependent endothelial function and reduces platelet activation in diabetic rats induced by Streptozocin. [6] Rosuvastatin displays cardioprotective effects in vivo. Rosuvastatin (80 mg) is shows to decrease infarct size and improve cardiac mechanical function after ischemia/reperfusion in animal model. The cardioprotective properties of Rosuvastatin may be due to the improvement of coronary blood flow, decrease in resistance of coronary arteries mediated by enhanced eNOS expression, and the subsequent increase in the production of vascular endothelial NO. [7] Rosuvastatin (2.0 mg/kg) attenuates left ventricular hypertrophy produced by transaortic constriction in mice through regulation of Racl protein and NADPH oxidase activities. [8]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (199.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+dd H2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 500.57
Formula

C22H28FN3O6S.1/2Ca

CAS No. 147098-20-2
Storage powder
in solvent
Synonyms N/A
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.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+2]

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04889287 Active not recruiting Drug: Elinzanetant (BAY3427080)|Drug: Rosuvastatin Vasomotor Symptoms as a Sex-hormone Dependent Disorder in Women and Men Bayer May 26 2021 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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HMG-CoA Reductase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID