1. Neuronal Signaling Stem Cell/Wnt
  2. γ-secretase
  3. MK-0752

MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.

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

MK-0752 Chemical Structure

MK-0752 Chemical Structure

CAS No. : 471905-41-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 288 In-stock
Solution
10 mM * 1 mL in DMSO USD 288 In-stock
Solid
1 mg USD 124 In-stock
5 mg USD 262 In-stock
10 mg USD 342 In-stock
50 mg USD 897 In-stock
100 mg USD 1357 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    MK-0752 purchased from MedChemExpress. Usage Cited in: Andrologia. 2019 Nov;51(10):e13413.  [Abstract]

    MK-0752 regulated the expression of cell proliferation-related genes at the mRNA and protein levels. The relative protein expression of p27 and p21Waf1/Cip1 in TM3 Leydig cells after treatment with 25 μM MK-0752 respectively. The representative Western blots for p27 and p21Waf1/Cip1 after treatment with MK-0752.

    MK-0752 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966.  [Abstract]

    Turnover of endogenous CD74 P8 is inhibited by RO4929079 and BMS-906024. Cell lysate Western blot of A20 cells treated with GSIs is developed with In-1 antibody. MK-0752 and Semagacestat tests used the same control lane (0 nM).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo[1][2].

    In Vivo

    MK-0752 (60-240 mg/kg; p.o.) decreases the generation of newly produced Aβ in the brain of rhesus monkeys[1].

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

    Animal Model: Male rhesus monkeys[1]
    Dosage: 60-240 mg/kg
    Administration: P.o.
    Result: Generation of new Aβ was partially blocked with administration of 60 mg/kg, and nearly completely blocked at the 240 mg/kg dose as indicated by the dose-dependent decrease in the amount of 13C6-leucine-labeled Aβ.
    Clinical Trial
    Molecular Weight

    442.90

    Formula

    C21H21ClF2O4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S([C@@]1(C2=C(C=CC(F)=C2)F)CC[C@@H](CCC(O)=O)CC1)(C3=CC=C(Cl)C=C3)=O

    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 : ≥ 100 mg/mL (225.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 10 mg/mL (22.58 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2578 mL 11.2892 mL 22.5785 mL
    5 mM 0.4516 mL 2.2578 mL 4.5157 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
    ×
    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

    ×
    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 (5.64 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 (5.64 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: 99.35%

    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
    Ethanol / DMSO 1 mM 2.2578 mL 11.2892 mL 22.5785 mL 56.4462 mL
    5 mM 0.4516 mL 2.2578 mL 4.5157 mL 11.2892 mL
    10 mM 0.2258 mL 1.1289 mL 2.2578 mL 5.6446 mL
    15 mM 0.1505 mL 0.7526 mL 1.5052 mL 3.7631 mL
    20 mM 0.1129 mL 0.5645 mL 1.1289 mL 2.8223 mL
    DMSO 25 mM 0.0903 mL 0.4516 mL 0.9031 mL 2.2578 mL
    30 mM 0.0753 mL 0.3763 mL 0.7526 mL 1.8815 mL
    40 mM 0.0564 mL 0.2822 mL 0.5645 mL 1.4112 mL
    50 mM 0.0452 mL 0.2258 mL 0.4516 mL 1.1289 mL
    60 mM 0.0376 mL 0.1882 mL 0.3763 mL 0.9408 mL
    80 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7056 mL
    100 mM 0.0226 mL 0.1129 mL 0.2258 mL 0.5645 mL
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    MK-0752 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.

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    Product Name:
    MK-0752
    Cat. No.:
    HY-10974
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