Shopping Cart
Remove All
  • TargetMol
    Your shopping cart is currently empty

Rosuvastatin

Copy Product Info
🥰Excellent
Catalog No. T1676Cas No. 287714-41-4
Alias ZD 4522

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

Rosuvastatin

Rosuvastatin

Copy Product Info
🥰Excellent
Purity: 99.95%
Catalog No. T1676Alias ZD 4522Cas No. 287714-41-4
Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$40In StockIn Stock
10 mg$59In StockIn Stock
25 mg$109In StockIn Stock
50 mg$166In StockIn Stock
100 mg$247In StockIn Stock
1 mL x 10 mM (in DMSO)$42In StockIn Stock
Add to Cart
Add to Quotation
In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Questions
TargetMol
View More

Batch Information

Select Batch
Purity:99.95%
Color:White to Yellow
Contact us for more batch information

Resource Download

Product Introduction

Rosuvastatin AI Summary
Rosuvastatin exhibits potent bioactivity primarily as an inhibitor of HMG-CoA reductase, displaying extremely low IC50 values across various models, indicating strong inhibition of cholesterol synthesis. In rat hepatocytes, it has a highly potent IC50 of 0.23 nM, while in liver microsomes, it shows an IC50 of approximately 3.1 nM. Studies demonstrate its varying potency across different cell types, including less effective inhibition in rat L6 myocytes with an IC50 of 250.0 nM. It also exhibits substantial inhibition in acute cholesterol synthesis in mice and reduces LDL cholesterol levels in multiple animal models. Pharmacokinetic assessments reveal significant bioavailability challenges, with only 20% oral bioavailability and substantial metabolism in the liver and intestines. Additionally, the compound undergoes extensive plasma protein binding and clearance in humans. Although showing modest antimalarial, antiviral, and antiproliferative activities, it possesses notable liver toxicity risks, as evidenced by predictions and clinical trial observations. Rosuvastatin also interacts with various human and rat hepatic transporters, influencing drug uptake and clearance rates in hepatic systems. Further, it affects permeability and transport interactions in cellular assays, including drug uptake ratios in hepatic and Caco-2 cells. These combined properties suggest Rosuvastatin holds potential as a robust hypolipidemic agent but necessitates careful consideration of its pharmacokinetic and toxicity profiles..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.
Targets&IC50
HMG-CoA:11 nM
In vitro
METHODS: Microglia cultures subDIV were treated with Rosuvastatin (1 µM) and LPS (20 ng/mL) for 24 h, and cell counts were measured by Bürker chamber.
RESULTS: After the 24 h treatment period, Rosuvastatin significantly inhibited cell proliferation in unchallenged and LPS-challenged cultures by 47.8% and 68.9%, respectively. [1]
METHODS: Nthy-ori 3-1 and B-CPAP cells were treated with Rosuvastatin (12.5-200 µM) for 48-72 h. Apoptosis was detected by TUNEL assay.
RESULTS: The number of apoptotic cells increased in both Nthy ori 3-1 and B-CPAP cells after Rosuvastatin treatment. 12.5 µM concentration of Rosuvastatin treatment resulted in an increase in Apoptotic Index of Nthy ori 3-1 and B-CPAP cells after 48 h. The results were summarized as follows. [2]
In vivo
METHODS: To investigate the anti-atherosclerotic effects, Rosuvastatin (5 mg/kg) and candesartan (2.5 mg/kg) were administered by gavage to streptozotocin-induced diabetic Apoe-/- mice once daily for 20 weeks.
RESULTS: In the absence of lipid-lowering effects, Rosuvastatin attenuated plaque area in diabetic mice.The anti-atherosclerotic effect of Rosuvastatin was comparable to that of candesartan. Dual therapy had similar beneficial effects, although it was not superior to monotherapy. [3]
SynonymsZD 4522
Chemical Properties
Molecular Weight481.54
FormulaC22H28FN3O6S
Cas No.287714-41-4
SmilesCC(C)c1nc(nc(-c2ccc(F)cc2)c1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)N(C)S(C)(=O)=O
Relative Density.1.368 g/cm3
Storage & Solubility Information
Storagekeep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 1 mg/mL (2.08 mM), Sonication is recommended.
DMSO: 50 mg/mL (103.83 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.0767 mL10.3834 mL20.7667 mL103.8335 mL
DMSO
1mg5mg10mg50mg
5 mM0.4153 mL2.0767 mL4.1533 mL20.7667 mL
10 mM0.2077 mL1.0383 mL2.0767 mL10.3834 mL
20 mM0.1038 mL0.5192 mL1.0383 mL5.1917 mL
50 mM0.0415 mL0.2077 mL0.4153 mL2.0767 mL
100 mM0.0208 mL0.1038 mL0.2077 mL1.0383 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy Rosuvastatin | purchase Rosuvastatin | Rosuvastatin cost | order Rosuvastatin | Rosuvastatin chemical structure | Rosuvastatin in vivo | Rosuvastatin in vitro | Rosuvastatin formula | Rosuvastatin molecular weight