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MLS6357

MLS6357 is a D3 dopamine receptor (D3R) -selective positive allosteric modulator (PAM) -antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM) . MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder[1].

Product Specifications

CAS Number

[932544-59-7]

UNSPSC

12352005

Target

Dopamine Receptor; PERK

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C(C1=C(NC(C)=C1S(NC2=CC(Cl)=C(C=C2)C)(=O)=O)C)N3CCCC3

Molecular Formula

C18H22ClN3O3S

Molecular Weight

395.90

References & Citations

[1]Moritz AE, et al. Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D3 Dopamine Receptor. J Med Chem. 2025 Aug 14;68 (15) :16691-16749.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

D1 Receptor; D2 Receptor; D3 Receptor; D4 Receptor; D5 Receptor

Curated Selection

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