MK-0752 471905-41-6

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

442.9 MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.






Biological Activity


MK-0752 is identified as a moderately potent γ-secretase inhibitor,
which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in
human SH-SY5Y cells. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation.


MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90%
decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752
treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while
decreases levels of Aβ 1-17. In guinea-pigs, oral
administration of MK-0752 (10 mg/kg -30 mg/kg) results in the
dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal
fluid (CSF) with IC50 of 440 nM in brain.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Contact us if you need more details on 471905-41-6. We are ready to answer your questions on packaging, logistics, certification or any other aspects about MK-0752 471905-41-6、471905-41-6 MK-0752. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Proteases > Gamma-secretase Inhibitor