M4 mAChR Modulator-2
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) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
For research use only. We do not sell to patients.
- CAS No.: 3062458-27-6
- Formula: C26H24FN5O
- Molecular Weight:441.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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mAChR4 513 nM (EC50) |
mAChR4 377 nM (Ki) |
M4 mAChR Modulator-2 (Compound A9) enhances acetylcholine-induced activation of M4 muscarinic acetylcholine receptors (M4 mAChR) (EC50 = 513 nM) in Cisbio IP-One Gq assay, showing potent M4 positive allosteric modulator (PAM) activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice[1]
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Dosage:10, 30, 60, 120 mg/kg
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Administration:p.o. administered 30 min before intraperitoneal injection of 0.3 mg/kg Dizocilpine (MK-801) (HY-15084B) for a single dose
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Result:Reversed MK-801-induced hyperlocomotion in male ICR mice with an ED₅₀ of 20.04 mg/kg (p.o.) when administered 30 min before intraperitoneal injection of 0.3 mg/kg MK-801, with locomotor activity recorded for 60 min.
Showed no adverse effects (including mortality, diarrhea, sedation, or gait abnormalities) in male ICR mice at the highest tested dose of 120 mg/kg.
Chemical Information
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CAS No. 3062458-27-6
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Molecular Weight 441.50
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Formula C26H24FN5O
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SMILES
CC1=C2C(CN(C(CC3CN(C4=CC(C5=CC=C(C#N)C(F)=C5)=NC=C4)C3)=O)C2)=NC(C)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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