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  3. Rosuvastatin

Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

For research use only. We do not sell to patients.

CAS No. : 287714-41-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Rosuvastatin:

Top Publications Citing Use of Products

    Rosuvastatin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jul 5:e2403451.  [Abstract]

    Western blotting of PAQR9 in mouse primary hepatocytes under the treatment of DMSO, simvastatin (Sim), atorvastatin (Ator), and rosuvastatin (Rosu) (10 μM; 24–48 h) was performed.

    Rosuvastatin purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Aug 31;5(9):e681.

    Chemerin levels in the medium of HepG2 cells cultured for 48 h, in the absence (control) or presence of atorvastatin, evolocumab, or Rosuvastatin, were measured.

    Rosuvastatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 May 29;10(1):263.  [Abstract]

    Rosuvastatin calcium (5 mg/kg i.p.) was administered. Images of the wound area in the rosuvastatin calcium-treated group and the control group were captured.

    Rosuvastatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 May 29;10(1):263.  [Abstract]

    Rosuvastatin calcium (5 mg/kg i.p.) was administered. The free cholesterol level of skin tissue after rosuvastatin calcium treatment for 12 days was measured. Each experiment was replicated at least thrice and representative images were shown.

    Rosuvastatin purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jul;44(7):1416-1428.  [Abstract]

    Rosuvastatin calcium (10 mg/kg body weight every second day, n = 5) was administered. The body weights of control and bavachin-treated mice were measured weekly from weeks 1 to 20.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3].

    IC50 & Target

    IC50: 11 nM (HMG-CoA), 195 nM (hERG)[1][2]

    Cellular Effect
    Cell Line Type Value Description References
    Hepatocyte IC50
    0.23 nM
    Compound: 1, rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocytes
    Inhibition of cholesterol synthesis in rat hepatocytes
    [PMID: 17764936]
    Hepatocyte IC50
    0.23 nM
    Compound: 26
    Inhibition of cholesterol synthesis in rat hepatocytes
    Inhibition of cholesterol synthesis in rat hepatocytes
    [PMID: 18540668]
    Hepatocyte IC50
    0.23 nM
    Compound: ros, rosuvastatin
    Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
    Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
    [PMID: 17560788]
    Hepatocyte IC50
    0.27 nM
    Compound: Rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocyte
    Inhibition of cholesterol synthesis in rat hepatocyte
    [PMID: 17574412]
    Hepatocyte IC50
    0.27 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocyte
    Inhibition of cholesterol synthesis in rat hepatocyte
    [PMID: 18155906]
    Hepatocyte IC50
    0.3 nM
    Compound: Rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocytes assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 4 hrs before addition of [14C]-acetic acid by liquid scintillation counting
    Inhibition of cholesterol synthesis in rat hepatocytes assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 4 hrs before addition of [14C]-acetic acid by liquid scintillation counting
    [PMID: 21183342]
    Hepatocyte IC50
    0.3 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocytes
    Inhibition of cholesterol synthesis in rat hepatocytes
    [PMID: 18072721]
    Hepatocyte IC50
    0.6 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol
    Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol
    [PMID: 18412317]
    L6 IC50
    210 nM
    Compound: 1, rosuvastatin
    Inhibition of cholesterol synthesis in L6 myocytes
    Inhibition of cholesterol synthesis in L6 myocytes
    [PMID: 17764936]
    L6 IC50
    250 nM
    Compound: Rosuvastatin
    Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
    Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
    [PMID: 21183342]
    L6 IC50
    250 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat L6 cells
    Inhibition of cholesterol synthesis in rat L6 cells
    [PMID: 18072721]
    L6 IC50
    250 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat L6 myocyte
    Inhibition of cholesterol synthesis in rat L6 myocyte
    [PMID: 18155906]
    L6 IC50
    65 nM
    Compound: rosuvastatin
    Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol
    Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol
    [PMID: 18412317]
    L6 IC50
    720 nM
    Compound: 26
    Inhibition of cholesterol synthesis in rat L6 myocytes
    Inhibition of cholesterol synthesis in rat L6 myocytes
    [PMID: 18540668]
    L6 IC50
    720 nM
    Compound: ros, rosuvastatin
    Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
    Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
    [PMID: 17560788]
    Ventricular myocyte IC50
    250 nM
    Compound: Rosuvastatin
    Inhibition of cholesterol synthesis in rat myocyte
    Inhibition of cholesterol synthesis in rat myocyte
    [PMID: 17574412]
    In Vivo

    Rosuvastatin (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms[2].
    Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    481.54

    Formula

    C22H28FN3O6S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C[C@H](O)C[C@H](O)/C=C/C1=C(C(C)C)N=C(N(C)S(=O)(C)=O)N=C1C2=CC=C(F)C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (207.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0767 mL 10.3834 mL 20.7667 mL
    5 mM 0.4153 mL 2.0767 mL 4.1533 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.67%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0767 mL 10.3834 mL 20.7667 mL 51.9168 mL
    5 mM 0.4153 mL 2.0767 mL 4.1533 mL 10.3834 mL
    10 mM 0.2077 mL 1.0383 mL 2.0767 mL 5.1917 mL
    15 mM 0.1384 mL 0.6922 mL 1.3844 mL 3.4611 mL
    20 mM 0.1038 mL 0.5192 mL 1.0383 mL 2.5958 mL
    25 mM 0.0831 mL 0.4153 mL 0.8307 mL 2.0767 mL
    30 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7306 mL
    40 mM 0.0519 mL 0.2596 mL 0.5192 mL 1.2979 mL
    50 mM 0.0415 mL 0.2077 mL 0.4153 mL 1.0383 mL
    60 mM 0.0346 mL 0.1731 mL 0.3461 mL 0.8653 mL
    80 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6490 mL
    100 mM 0.0208 mL 0.1038 mL 0.2077 mL 0.5192 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Rosuvastatin
    Cat. No.:
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