MLS1547

MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM) . MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay) . MLS1547 acts as an antagonist for dopamine (DA) -stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM) [1][2].

Product Specifications

CAS Number

[315698-36-3]

UNSPSC

12352005

Hazard Statement

H301

Target

Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/mls1547.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

OC1=C2N=CC=CC2=C(Cl)C=C1CN3CCN(C4=NC=CC=C4)CC3

Molecular Formula

C19H19ClN4O

Molecular Weight

354.83

Precautions

H301

References & Citations

[1]Free RB, et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol. 2014;86 (1) :96-105.|[2]Chun LS, et al. Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor. Front Synaptic Neurosci. 2018;10:2. Published 2018 Feb 21.