656810-87-6
Chemical Structure
MK-0752 sodium
- CAS No.: 656810-87-6
- Formula:C21H20ClF2NaO4S
- Molecular Weight:464.89
IUPAC Name: sodium 3-((1s,4r)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoate
InChIKey: WFPVQMLUYJLUCN-YQEPSNHFSA-M
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]
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
