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M4 mAChR Modulator-2

CAT: 0931-T212236-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T212236-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
3062458-27-6
Target
AChR
Related Pathways
Neuroscience
Bioactivity
M4mAChRModulator-2 is an orally active and selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4mAChR) capable of crossing the blood-brain barrier, with an EC50 of 513 nM. It demonstrates high target selectivity, showing minimal 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 M4mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. Additionally, M4mAChRModulator-2 can reverse the hyperlocomotion induced by Dizocilpine (MK-801) in mice and is applicable for schizophrenia research.
Smiles
N#CC=1C=CC(=CC1F)C2=NC=CC(=C2)N3CC(CC(=O)N4CC5=NC(=CC(=C5C4)C)C)C3
Molecular Formula
C26H24FN5O
Molecular Weight
441.5
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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