Rosuvastatin

Catalog No.S5072

Rosuvastatin Chemical Structure

Molecular Weight(MW): 481.54

Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, with Ki value (inhibition constant) of approximately 0.1 nM.

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Biological Activity

Description Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, with Ki value (inhibition constant) of approximately 0.1 nM.
Targets
HMG-CoA reductase [1]
()
In vitro

Rosuvastatin possesses a greater number of binding interactions with HMG-CoA reductase and has a high affinity for the active site of the enzyme. Rosuvastatin is relatively hydrophilic and is selectively taken up by, and active in, hepatic cells. Rosuvastatin has the longest terminal half-life of the statins and is only minimally metabolized by the cytochrome P450 (CYP 450) enzyme system with no significant involvement of the 3A4 enzyme[2].

In vivo Rosuvastatin attenuates arterial thrombosis and neointima formation, and it may stabilise vascular lesions developing after endothelial injury in mice. These effects are independent of systemic lipid lowering[3].

Protocol

Animal Research:

[1]

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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: 0.9% NaCl
  • Dosages: 0.125, 0.25, or 1.25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.36 mM)
Water 96 mg/mL (199.36 mM)
Ethanol 23 mg/mL (47.76 mM)

* 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 481.54
Formula

C22H28FN3O6S
 

CAS No. 287714-41-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02662894 Not yet recruiting Hypertension|Dyslipidemia EMS October 2019 Phase 3
NCT02662894 Not yet recruiting Hypertension|Dyslipidemia EMS October 2019 Phase 3
NCT03872232 Active not recruiting Hypercholesterolemia|Hypertension Addpharma Inc. February 26 2019 Phase 3
NCT03526367 Not yet recruiting Contrast-induced Acute Kidney Injury|ST Elevation Myocardial Infarction|Primary PCI|Rosuvastatin|Hydration Shenyang Northern Hospital February 20 2019 Phase 4
NCT03872232 Active not recruiting Hypercholesterolemia|Hypertension Addpharma Inc. February 26 2019 Phase 3
NCT03526367 Not yet recruiting Contrast-induced Acute Kidney Injury|ST Elevation Myocardial Infarction|Primary PCI|Rosuvastatin|Hydration Shenyang Northern Hospital February 20 2019 Phase 4

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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