VU0448088 (Synonyms: ML253)

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VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC₅₀ values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic.

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

VU0448088 Chemical Structure

CAS No. : 1417616-42-2

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

mAChR4

56 nM (EC₅₀)

In Vivo

VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) reverses amphetamine-induced hyperlocomotion in a dose-dependent manner ^[1].

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

Animal Model:	Rat (amphetamine-induced hyperlocomotion)^[1]
Dosage:	3, 10, 30, 56.6, 100 mg/kg
Administration:	IP
Result:	Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, showed a modest reduction of 26% at a dose of 10 mg/kg; at the three highest doses (30, 56.6 and 100 mg/kg), showed significant reductions of 47.9%, 53.7% and 57.3%, respectively.

Molecular Weight

346.83

Formula

C₁₆H₁₅ClN₄OS

CAS No.

1417616-42-2

SMILES

CC1=C(Cl)C(C)=NC2=C1C(N)=C(C(NCC3=CC=NC=C3)=O)S2

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]. Le U, et al. Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett. 2013 Jan 1;23(1):346-50. [Content Brief]

VU0448088 Related Classifications

Neurological Disease

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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:

VU04480881417616-42-2ML253VU 0448088VU-0448088ML 253ML-253mAChRMuscarinic acetylcholine receptorblood-brain barrierpsychoticamphetamineInhibitorinhibitorinhibit

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