| Bioactivity | MK-0752 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 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo[1][2]. | ||||||||||||
| In Vivo | MK-0752 (60-240 mg/kg; p.o.) decreases the generation of newly produced Aβ in the brain of rhesus monkeys[1]. Animal Model: | ||||||||||||
| Name | MK-0752 | ||||||||||||
| CAS | 471905-41-6 | ||||||||||||
| Formula | C21H21ClF2O4S | ||||||||||||
| Molar Mass | 442.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |