MK-6884

• CAT Number: I032394
• CAS Number: 2102194-04-5
• Molecular Formula: C25H25N5O
• Molecular Weight: 411.50
• Purity: ≥95%
• Synonyms: 5-[1-[(1-methylcyclopentyl)methyl]pyrazol-4-yl]-6-(2-methyl-3-oxo-1H-isoindol-5-yl)pyridine-2-carbonitrile
• InChI: InChI=1S/C25H25N5O/c1-25(9-3-4-10-25)16-30-15-19(13-27-30)21-8-7-20(12-26)28-23(21)17-5-6-18-14-29(2)24(31)22(18)11-17/h5-8,11,13,15H,3-4,9-10,14,16H2,1-2H3
• InChIKey: PREPVVXBTJBVOZ-UHFFFAOYSA-N
• SMILES: CC1(CCCC1)CN2C=C(C=N2)C3=C(N=C(C=C3)C#N)C4=CC5=C(CN(C5=O)C)C=C4

MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent[1].
MK-6884 (compound 13; 0-22 µM) is a PAM of ACh function in a cell-based Ca2+ mobilization assay, with an EC50 of 27 nM[1].
[11C]MK-6884 (compound 13) shows non-displaceable binding potential (BPND) of 0.83 in rhesus monkeys[1].
[11C]MK-6884 (approximately 185 MBq, <2 μg; single intravenous) distributes on the known presence of M4 receptors in the rhesus monkeys brain[1]. [11C]MK-688 can penetrate the blood-brain barrier in monkeys[1].

Reference

[1]. Tong L, et al. Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases. J Med Chem. 2020;63(5):2411-2425.
 [Content Brief]