11C-MK-3168

Names

[ CAS No. ]:
1242441-58-2

[ Name ]:
11C-MK-3168

Biological Activity

[Description]:

11C-MK-3168 is a potent, reversible and blood/brain barrier penetrated fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, respectively.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> FAAH
Signaling Pathways >> Neuronal Signaling >> FAAH
Research Areas >> Others

[Target]

IC50: 1.0 nM (Human FAAH), 1.7 nM (Rat FAAH), 5.5 nM (Rhesus FAAH)[1]


[In Vitro]

11C-MK-3168 is a potent and reversible fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, respectively. 11C-MK-3168 also shows selectivity over hERG (IC50 = 37 μM) and DLZ (IC50 = 16 μM); CYP 3A4 (IC50 > 50 μM); and the two cannabinoid receptors, CB1 (IC50 = 30 μM) and CB2 (IC50 = 150 μM)[1].

[References]

[1]. Liu P, et al. Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase. ACS Med Chem Lett. 2013 Apr 20;4(6):509-13.


[Related Small Molecules]

BIA 10-2474 | PF-04457845 | URB597 | biochanin A | JZL195 | PF-3845 | LY2183240 | JNJ-42165279 | FAAH-IN-2 | Macamide B | FAAH inhibitor 1 | FAAH-IN-1 | SA72

Chemical & Physical Properties

[ Molecular Formula ]:
C2011CH21ClN4OS

[ Molecular Weight ]:
411.94


Related Compounds