2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis
  4. Pitavastatin

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

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CAS No. : 147511-69-1

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Pitavastatin:

Pitavastatin Related Antibodies

Top Publications Citing Use of Products

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 May 29;13(6):667.  [Abstract]

    Pitavastatin Calcium (0.5-1 μM) makes FLC fungicidal.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 May 29;13(6):667.  [Abstract]

    PIT (0-25 μM) confers fungicidal properties to voriconazole, ketoconazole, itraconazole, and miconazole.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 May 29;13(6):667.  [Abstract]

    MIC assays and spotting assays show that erg11△/erg11△ was significantly sensitive to PIT (0-100 μM) compared to the wild-type strain.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2024 Jun:147:107369.  [Abstract]

    Oil red O staining and quantification of zebrafish liver after treatment with DTPP and Pitavastatin Calcium. Day1 of DTPP treatment.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2024 Jun:147:107369.  [Abstract]

    Oil red O staining and quantification of zebrafish liver after treatment with DTPP and Pitavastatin Calcium. Day3 of DTPP treatment.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2024 Apr 25;56(4):621-633.  [Abstract]

    Typical oil red O staining images showing the alleviation of lipid accumulation by LMY and Pitavastatin (NK-104) (2% (w/w); dietary administration) in larval zebrafish. The number of zebrafish larvae involved in each experimental group is indicated in the top left corner of each image.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Proteomics. 2023 Aug;23(16):e2300041.  [Abstract]

    IC50 values of ERK, S6K inhibitors and statins in parental and resistant cells. (The treatment duration for compounds such as Pitavastatin was 72 h.)

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Proteomics. 2023 Aug;23(16):e2300041.  [Abstract]

    Western blot against cav-1 after treatment of resistant cells with statins at IC50s for 48 h. Stained MIA PaCa-2 cells were treated with 1 µM GDC-0994, 30 µM DG2, 1.56 µM atorvastatin, 1.56 µM fluvastatin or 0.195 µM Pitavastatin.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):850-860.  [Abstract]

    Pharmacokinetic parameters of Pitavastatin (5 mg/kg; single dose) after oral administration.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):850-860.  [Abstract]

    Pharmacokinetics of Pitavastatin (5 mg/kg; p.o.; single dose) in WT and KO rats. The concentrations of Pitavastatin were determined by LC–MS/MS.

    Pitavastatin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2019 Nov:169:113612.  [Abstract]

    Uptake ability of Pitavastatin (a human OATP1B1/1B3 substrate，0.1-10 μM; 1 h) by the control and rSlco1b2 overexpression cells. The rate was expressed as the relative intracellular substrate concentration (substrate/internal standard MS/MS response ratio).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects[1][2][3][8].

    IC50 & Target

    HMG-CoA Reductase[1]
    In Vitro

    Pitavastatin inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50=0.4-5 μM) or as spheroids (IC50 = 0.6-4 μM)[4]. 
    Pitavastatin (1 μM; 48 hours) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[4].
    Pitavastatin (1 μM, 48 hours) causes PARP cleavage in Ovcar-8 cells[4].
    Pitavastatin (0.1 and 1 μM; 1 h, then cells incubate with TNF-α for 6 h) increases the expression of ICAM-1 mRNA through suppressing NF-κB pathway in TNF-α-stimulated human saphenous vein endothelial cells[6].

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

    Pitavastatin Related Antibodies

    Western Blot Analysis[4]

    Cell Line: Ovcar-8 cells
    Concentration: 1 μM
    Incubation Time: 48 hours
    Result: Induced PARP cleavage.
    In Vivo

    Pitavastatin (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression[4].
    Pitavastatin (0.1 mg/kg; p.o; daily for 12 weeks) retards the progression of atherosclerosis formation and improves NO bioavailability by eNOS up-regulation and decrease of O2- in diet induced severe hyperlipidemia rabbit model[7].

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

    Animal Model: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours)[4]
    Dosage: 59 mg/kg
    Administration: p.o.; twice daily for 28 days
    Result: Caused significant tumour regression.
    Animal Model: Female New Zealand white rabbits (diet induced severe hyperlipidemia)[7]
    Dosage: 0.1 mg/kg
    Administration: p.o; daily for 12 weeks
    Result: Retarded the progression of atherosclerosis formation and improved NO bioavailability by eNOS up-regulation and decrease of O2-.
    Molecular Weight

    421.46

    Formula

    C25H24FNO4
    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(C2=CC=C(F)C=C2)C3=CC=CC=C3N=C1C4CC4
    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 (237.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3727 mL 11.8635 mL 23.7270 mL
    5 mM 0.4745 mL 2.3727 mL 4.7454 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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 (5.93 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    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: 98.87%

    SDS (393 KB)

    COA (250 KB) HNMR (557 KB) LCMS (127 KB)

    Handling Instructions (2659 KB)
    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 2.3727 mL 11.8635 mL 23.7270 mL 59.3176 mL
    5 mM 0.4745 mL 2.3727 mL 4.7454 mL 11.8635 mL
    10 mM 0.2373 mL 1.1864 mL 2.3727 mL 5.9318 mL
    15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9545 mL
    20 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.9659 mL
    25 mM 0.0949 mL 0.4745 mL 0.9491 mL 2.3727 mL
    30 mM 0.0791 mL 0.3955 mL 0.7909 mL 1.9773 mL
    40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4829 mL
    50 mM 0.0475 mL 0.2373 mL 0.4745 mL 1.1864 mL
    60 mM 0.0395 mL 0.1977 mL 0.3955 mL 0.9886 mL
    80 mM 0.0297 mL 0.1483 mL 0.2966 mL 0.7415 mL
    100 mM 0.0237 mL 0.1186 mL 0.2373 mL 0.5932 mL
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    Pitavastatin Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

    Keywords:

    Pitavastatin147511-69-1NK-104NK104NK 104HMG-CoA Reductase (HMGCR)AutophagyMitophagyApoptosisMitochondrial Autophagyanti-atheroscleroticanti-asthmaticanti-osteoarthritisantineoplasticneuroprotectivehepatoprotectivereno-protectiveInhibitorinhibitorinhibit

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