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Signal Inhibitors and Activators
MK-0752
$816/ 5mg
QuantityTotal: $816
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Product Information
Kinase Inhibitor Name MK-0752
FormulaC21H21ClF2O4S
SolubilityDMSO ≥89 mg/mL Water <1 mg/mL Ethanol ≥45 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.471905-41-6
Biological ActivityMK-0752 is a potent gamma secretase (γ-secretase) inhibitor in clinical development with an IC50 of 5 nM for Aβ40 in human SH-SY5Y cells.Defining the metabolic fate of amyloid precursor protein (APP) in the central nerve system (CNS) is critically important for the development of γ-secretase inhibitors to treat Alzheimer’s disease (AD), as a substrate build-up of APP fragments could potentially lead to an overshoot in neurotoxic amyloid peptides. The lack of Aβ rebound in the CNS could be attributed to the shunting of APP (possibly beta C-terminal fragments, e.g. C99) to γ-secretase independent degradation. MK-0752 reduced Aβ40 in a dose-dependent manner. Dose-dependent reductions in plasma, brain and CSF Aβ40 were observed in guinea-pigs following single oral doses of 10–30 mg/kg (brain IC50 = 0.44 μM). [1][2]
M.W.442.9
ReferencesDetermination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). Bai F et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52.
Recent progress in the medicinal chemistry of gamma-secretase inhibitors. Olson RE et al. Curr Top Med Chem. 2008;8(1):17-33.
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. Cook JJ et al. J Neurosci. 2010 May 12;30(19):6743-50.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Recent progress in the medicinal chemistry of gamma-secretase inhibitors. Olson RE et al. Curr Top Med Chem. 2008;8(1):17-33.
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. Cook JJ et al. J Neurosci. 2010 May 12;30(19):6743-50.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Price816$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
gamma secretase (γ-secretase) inhibitor in clinical development SH-SY5Y cells.Defining the metabolic fate of amyloid precursor (CNS) is critically important for the development of γ-secretase (AD), as a substrate build-up of APP fragments could amyloid peptides. The lack of Aβ rebound in the CNS could beta C-terminal fragments, e.g. C99) to γ-secretase independent
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