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M4 mAChR Modulator-2

🥰Excellent
Catalog No. T212236Cas No. 3062458-27-6

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.

M4 mAChR Modulator-2

M4 mAChR Modulator-2

🥰Excellent
Catalog No. T212236Cas No. 3062458-27-6
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.
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Product Introduction

Bioactivity
Description
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.
Targets&IC50
M4 mAChR:513 nM (EC50)
In vitro
M4 mAChR Modulator-2 (Compound A9) potentiates acetylcholine-induced activation of the M4 muscarinic acetylcholine receptor (M4 mAChR) with an EC50 of 513 nM, as observed in the Cisbio IP-One Gq assay, demonstrating strong activity as a positive allosteric modulator (PAM) of M4.
In vivo
M4 mAChR Modulator-2 (Compound A9), administered orally at doses of 10-120 mg/kg, counteracts MK-801 (0.3 mg/kg, intraperitoneal) induced hyperactivity in male ICR mice when given 30 minutes prior to MK-801.
Chemical Properties
Molecular Weight441.50
FormulaC26H24FN5O
Cas No.3062458-27-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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