Bioactivity | 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]. |
CAS | 656810-87-6 |
Formula | C21H20ClF2NaO4S |
Molar Mass | 464.89 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |