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Art. -Nr.: HY-175532

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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 K_i 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. Nr.: 3062458-27-6
Formel: C₂₆H₂₄FN₅O
Molecular Weight:441.50

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

M4 mAChR Modulator-2 Chemical Structure

CAS. Nr.: 3062458-27-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

mAChR4

513 nM (EC₅₀)

mAChR4

377 nM (Ki)

Alle mAChR Isoform-spezifische Produkte anzeigen :

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

Species	Dose	Route	T_1/2	C_max	AUC_inf	MRT_last	F
Rat^[1]	1 mg/kg	i.v.	0.95 h	1990 ng/mL	1970 ng·h/mL	1.10 h	/
Rat^[1]	10 mg/kg	p.o.	2.04 h	6290 ng/mL	18900 ng·h/mL	2.66 h	79.3 %

In Vivo

M4 mAChR Modulator-2 (Compound A9) (10-120 mg/kg p.o., administered 30 min before intraperitoneal injection of 0.3 mg/kg Dizocilpine (MK-801) (HY-15084B), single dose) reverses MK-801-induced hyperlocomotion in male ICR mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male ICR mice^[1]
Dosage:

10, 30, 60, 120 mg/kg
Administration:

p.o. administered 30 min before intraperitoneal injection of 0.3 mg/kg Dizocilpine (MK-801) (HY-15084B) for a single dose
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

CAS. Nr. 3062458-27-6
Molecular Weight 441.50
Formel C₂₆H₂₄FN₅O
SMILES

CC1=C2C(CN(C(CC3CN(C4=CC(C5=CC=C(C#N)C(F)=C5)=NC=C4)C3)=O)C2)=NC(C)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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M4 mAChR Modulator-2

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

M4 mAChR Modulator-2 Related Classifications

HY-175532 Related Classifications