My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    MK-0752
    MK-0752

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0717
    CAS #: 471905-41-6 Purity ≥98%

    Description: MK0752 (MK0752; MK-0752) is a novel, potent and synthetic small molecule inhibitor of γ-secretase (gamma-secretase). It reduces Aβ40 production with an IC50 of 5 nM and has potential anti-AD (Alzheimer's disease) and antineoplastic activity.

    References: J Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18.

    Related CAS: 656810-87-6 (sodium salt)

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)442.9
    FormulaC21H21ClF2O4S
    CAS No.471905-41-6 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (200.9 mM)
    Water: <1 mg/mL
    Ethanol: 45 mg/mL (101.6 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsMK0752; MK 0752; MK-0752 

    Chemical Name: 3-((1r,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid.

    InChi Key: XCGJIFAKUZNNOR-HNSKJHPRSA-N

    InChi Code: InChI=1S/C21H21ClF2O4S/c22-15-2-5-17(6-3-15)29(27,28)21(18-13-16(23)4-7-19(18)24)11-9-14(10-12-21)1-8-20(25)26/h2-7,13-14H,1,8-12H2,(H,25,26)/t14-,21-

    SMILES Code: O=C(O)CC[[email protected]]1CC[[email protected]](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

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

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

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

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation.


    Kinase Assay: MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. 


    Cell Assay: As a moderately potent γ-secretase inhibitor, MK-0752 inhibited the production of Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells.

    In VivoMK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain.
    Animal modelCisterna Magna Ported (CMP) Rhesus Monkey Model.
    Formulation & DosageDissolved in water;  ≤240 mg/kg; Oral gavage
    ReferencesJ Neurosci. 2010 May 12;30(19):6743-50; Cancer Res. 2010 Jan 15;70(2):709-18.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    MK-0752
    Plasma levels of Aβ during and after γ-secretase inhibition indicate peripheral Aβ rebound in rhesus monkeys treated with a CNS-penetrant gamma secretase inhibitor (GSI MK0752). J Neurosci. 2010 May 12;30(19):6743-50.
     
    MK-0752MK-0752MK-0752
    No evidence of central Aβ rebound in rhesus monkeys treated with a CNS-penetrant γ-secretase inhibitor (GSI). J Neurosci. 2010 May 12;30(19):6743-50.
     
    MK-0752
    Newly generated Aβ was reduced in response to g-secretase inhibitor (GSI) treatment in the CNS of rhesus monkeys (n=6). J Neurosci. 2010 May 12;30(19):6743-50.
     
    MK-0752
    γ-secretase inhibition modulates levels of Aβ 1–14, 1–15, 1–16 and 1–17. J Neurosci. 2010 May 12;30(19):6743-50.



    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?