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
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- CAS No.: 3062458-27-6
- Formule: C26H24FN5O
- Masse moléculaire:441.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
mAChR4 513 nM (EC50) |
mAChR4 377 nM (Ki) |
In Vitro
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.
Parmacokinetics
In Vivo
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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Masse moléculaire 441.50
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M4 mAChR Modulator-2 Related Classifications
HY-175532 Related Classifications
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