| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | [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]. | ||||||||||||
| Name | MK-6884 | ||||||||||||
| CAS | 2102194-04-5 | ||||||||||||
| Formula | C25H25N5O | ||||||||||||
| Molar Mass | 411.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |