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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
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.
Targets |
Aβ (IC50 = 5 nM)
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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]
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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]
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Enzyme Assay |
MK-0752 is a γ-secretase inhibitor of moderate potency that decreases the production of Aβ40 at an IC50 of 5 nM.
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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.
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Animal Protocol |
Cisterna Magna Ported (CMP) Rhesus Monkey Model.
≤240 mg/kg Administered via p.o. |
References |
Molecular Formula |
C21H21CLF2O4S
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Molecular Weight |
442.9
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Exact Mass |
442.902
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Elemental Analysis |
C, 56.95; H, 4.78; Cl, 8.00; F, 8.58; O, 14.45; S, 7.24
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CAS # |
471905-41-6
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Appearance |
Solid powder
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SMILES |
C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
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InChi Key |
XCGJIFAKUZNNOR-UHFFFAOYSA-N
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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)
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Chemical Name |
3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid
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Synonyms |
MK0752; MK 0752; MK-0752
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
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 |