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M4 mAChR Modulator-2

CAT: 0804-HY-175532Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-175532Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) -induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia[1]
CAS Number
3062458-27-6
UNSPSC
12352005
Target
MAChR
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Smiles
CC1=C2C(CN(C(CC3CN(C4=CC(C5=CC=C(C#N)C(F)=C5)=NC=C4)C3)=O)C2)=NC(C)=C1
Molecular Formula
C26H24FN5O
Molecular Weight
441.50
References & Citations
[1]Luo Y, et al. Design, synthesis, and pharmacological evaluation of novel M4 muscarinic receptor positive allosteric modulators for schizophrenia treatment. Eur J Med Chem. 2025 Nov 15;298:117993.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MAChR4

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