1. Metabolic Enzyme/Protease Autophagy
  2. Phosphodiesterase (PDE) Autophagy
  3. Cilostazol

Cilostazol  (Synonyms: OPC 13013)

Cat. No.: HY-17464 Purity: 99.96%
COA Handling Instructions

Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.

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

Cilostazol Chemical Structure

Cilostazol Chemical Structure

CAS No. : 73963-72-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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100 mg USD 99 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Cilostazol:

Top Publications Citing Use of Products

    Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647.  [Abstract]

    Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model. The protein expression is detected by western blotting, and cell proliferation was analyzed by DAPI/Brdu staining.

    Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647.  [Abstract]

    Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in HUVEC H/I cell model.

    Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647.  [Abstract]

    Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model.

    Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647.  [Abstract]

    Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model. The protein expression is detected by western blotting, and cell proliferation was analyzed by DAPI/Brdu staining.

    View All Phosphodiesterase (PDE) Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].

    IC50 & Target

    IC50: 0.2 μM ( PDE 3A)[1]

    In Vitro

    Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists[2].
    Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-dependently, with an IC50 of 15 μM for SIPA, and with a similar IC50 of 12.5 μM for ADP-induced platelet aggregation[2].
    Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells[3].

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

    In Vivo

    Cilostazol (clinically used doses; p.o.; for 2 weeks) could alleviate CCl4 -induced hepatic fibrogenesis in vivo, presumably due to its direct effect to suppress HSC activation[3].
    Cilostazol (intraperitoneal injection; 10 mg/kg; 7 consecutive days after ischemia) attenuates neurological dysfunctions, brain atrophy and infarct volume, and inhibits astrocyte proliferation/glial scar formation and accelerated the angiogenesis in the ischemic boundary zone 7 and 28 days after ischemia[4].

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

    Animal Model: Male C57BL/6J mice[3]
    Dosage: 0.1% w/w, 0.3% w/w
    Administration: Oral administration; fed a normal diet for 2 weeks
    Result: Exhibited a lesser fibrotic area than control groups.
    Animal Model: Male ICR mice[4]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 7 consecutive days after ischemia
    Result: Had an effectve effects for the late injury.
    Clinical Trial
    Molecular Weight

    369.46

    Formula

    C20H27N5O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 50 mg/mL (135.33 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 2.7067 mL 13.5333 mL 27.0665 mL
    5 mM 0.5413 mL 2.7067 mL 5.4133 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2 mg/mL (5.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.96%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7067 mL 13.5333 mL 27.0665 mL 67.6663 mL
    5 mM 0.5413 mL 2.7067 mL 5.4133 mL 13.5333 mL
    10 mM 0.2707 mL 1.3533 mL 2.7067 mL 6.7666 mL
    15 mM 0.1804 mL 0.9022 mL 1.8044 mL 4.5111 mL
    20 mM 0.1353 mL 0.6767 mL 1.3533 mL 3.3833 mL
    25 mM 0.1083 mL 0.5413 mL 1.0827 mL 2.7067 mL
    30 mM 0.0902 mL 0.4511 mL 0.9022 mL 2.2555 mL
    40 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
    50 mM 0.0541 mL 0.2707 mL 0.5413 mL 1.3533 mL
    60 mM 0.0451 mL 0.2256 mL 0.4511 mL 1.1278 mL
    80 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8458 mL
    100 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6767 mL
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    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.

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    Product Name:
    Cilostazol
    Cat. No.:
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