MK-0752 (sodium)

MK-0752 sodium 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 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo[1][2].

Product Specifications

CAS Number

[656810-87-6]

UNSPSC

12352005

Target

γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/mk-0752-sodium.html

Smiles

O=C(CC[C@H]1CC[C@@](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1)O[Na]

Molecular Formula

C21H20ClF2NaO4S

Molecular Weight

464.89

References & Citations

[1]Cook JJ, et al. 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. J Neurosci. 2010;30 (19) :6743-6750.|[2]Krop I, et al. Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors. J Clin Oncol. 2012;30 (19) :2307-2313.