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MK-6884

Cat. No. M21257
MK-6884 Structure
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Biological Activity

MK-6884 is an M4 muscarinic receptor orthomodulator (PAM) with a Ki value of 0.19 nM. MK-6884 is used in the study of neurodegenerative diseases. MK-6884 can be used as a positron emission computed tomography imaging agent with 11C radiolabeling.

Chemical Information
Molecular Weight 411.50
Formula C25H25N5O
CAS Number 2102194-04-5
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Wenping Li, et al. Sci Transl Med. The PET tracer [11C]MK-6884 quantifies M4 muscarinic receptor in rhesus monkeys and patients with Alzheimer's disease

[2] Ling Tong, et al. J Med Chem. 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

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