MK-0752

Alias: MK0752; MK 0752; MK-0752
Cat No.:V0717 Purity: ≥98%
MK0752 (MK0752; MK-0752) is a novel, potent and synthetic small molecule inhibitor of γ-secretase (gamma-secretase).
MK-0752 Chemical Structure CAS No.: 471905-41-6
Product category: Gamma-secretase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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

Biological Activity I Assay Protocols (From Reference)
Targets
Aβ (IC50 = 5 nM)
ln Vitro
MK-0752 has been found to be a moderately potent inhibitor of γ-secretase, reducing Aβ40 in human SH-SY5Y cells in a dose-dependent manner with an IC50 of 5 nM. (Source: ) MK-0752 prevents the cleavage of the Notch-intracellular domain (ICD) and the ensuing nuclear translocation in vitro.[2]
ln Vivo
MK-0752 lowers AUV in the brains of rhesus monkeys by 90% while also reducing the production of newly formed Aβ. Furthermore, Aβ 1-17 levels are decreased while Aβ 1-14, Aβ 1-15, and Aβ 1-16 levels are increased with MK-0752 treatment. (Source: ) When given orally to guinea pigs, MK-0752 (10 mg/kg -30 mg/kg) reduces Aβ40 in plasma, brain, and cerebrospinal fluid (CSF) in a dose-dependent manner, with an IC50 of 440 nM in the brain.[2]
Enzyme Assay
MK-0752 is a γ-secretase inhibitor of moderate potency that decreases the production of Aβ40 at an IC50 of 5 nM.
Cell Assay
MK-0752, a moderately potent γ-secretase inhibitor, exhibited dose-dependent inhibition of Aβ40 production in human SH-SY5Y cells, with an IC50 of 5 nM.
Animal Protocol
Cisterna Magna Ported (CMP) Rhesus Monkey Model.
≤240 mg/kg
Administered via p.o.
References

[1]. J Neurosci . 2010 May 12;30(19):6743-50.

[2]. Cancer Res . 2010 Jan 15;70(2):709-18.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H21CLF2O4S
Molecular Weight
442.9
Exact Mass
442.902
Elemental Analysis
C, 56.95; H, 4.78; Cl, 8.00; F, 8.58; O, 14.45; S, 7.24
CAS #
471905-41-6
Appearance
Solid powder
SMILES
C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
InChi Key
XCGJIFAKUZNNOR-UHFFFAOYSA-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)
Chemical Name
3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid
Synonyms
MK0752; MK 0752; MK-0752
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.2258 mL 1.1289 mL 2.2578 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00803894 Completed Drug: MK0752
Drug: Comparator: Placebo
Healthy Merck Sharp & Dohme LLC December 2008 Phase 1
NCT01295632 Completed Drug: ridaforolimus
Drug: MK-0752
Advanced Cancer Merck Sharp & Dohme LLC February 2011 Phase 1
NCT00756717 Completed Drug: MK-0752 Breast Cancer Loyola University February 14, 2008 Phase 4
NCT00645333 Completed Drug: MK-0752, Docetaxel,
Pegfilgrastim
Metastatic Breast Cancer University of Michigan Rogel
Cancer Center
March 2008 Phase 1
Phase 2
Biological Data
Contact Us