VU6004256

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VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC₅₀ value of 155 nM. VU6004256 has the potential for the research of schizophrenia.

For research use only. We do not sell to patients.

VU6004256 Chemical Structure

CAS No. : 2011034-33-4

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Purity & Documentation
References
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Description

VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC₅₀ value of 155 nM. VU6004256 has the potential for the research of schizophrenia^[1].

IC₅₀ & Target^[1]

mAChR1

155 nM (EC₅₀)

In Vivo

VU6004256 (10 mg/kg; i.p.) attenuates excessive pyramidal cell firing in the prefrontal cortex of NR1 KD mice^[1].
VU6004256 (3, 10 mg/kg; i.p.) reverses the performance impairments in novel object recognition and cue-mediated fear conditioning tasks and reduces hyper locomotor activity in NR1 KD mice^[1].

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

Animal Model:	Adult male NR1 KD mice^[1]
Dosage:	10 mg/kg
Administration:	I.p.
Result:	Showed no effect on pyramidal cell firing rate in WT littermate controls, significantly reduced pyramidal cell firing rate in NR1 KD mice.

Animal Model:	Wild-type and NR1 KD mice^[1]
Dosage:	3, 10 mg/kg
Administration:	I.p.
Result:	Dose-dependently reduced locomotor activity in NR1 KD, but not in WT mice, resulted in dose-dependent increases in recognition index in WT and NR1 KD mice; improved performance on test day in cue-mediated conditioned freezing in NR1 KD but not WT mice.

Molecular Weight

465.50

Formula

C₂₅H₂₅F₂N₅O₂

CAS No.

2011034-33-4

SMILES

O=C(C1=CN(CC2=CC=C(C3=CN(C)N=C3)N=C2)C4=C1C(F)=CC(F)=C4)N[C@@H]5[C@@H](O)CCCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Grannan MD, et al. Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256. ACS Chem Neurosci. 2016 Dec 21;7(12):1706-1716. [Content Brief]

VU6004256 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU60042562011034-33-4VU 6004256VU-6004256mAChRMuscarinic acetylcholine receptorschizophreniaNR1 KD micenovel object recognitioncue-mediated fearhyper locomotor activityInhibitorinhibitorinhibit

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