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).

Product information

CAS Number: 315698-36-3

Molecular Weight: 354.83

Formula: C19H19ClN4O

Chemical Name: 5-chloro-7-{[4-(pyridin-2-yl)piperazin-1-yl]methyl}quinolin-8-ol

Smiles: OC1=C2N=CC=CC2=C(Cl)C=C1CN1CCN(CC1)C1=CC=CC=N1

InChiKey: OPEJNANYABTIGC-UHFFFAOYSA-N

InChi: InChI=1S/C19H19ClN4O/c20-16-12-14(19(25)18-15(16)4-3-7-22-18)13-23-8-10-24(11-9-23)17-5-1-2-6-21-17/h1-7,12,25H,8-11,13H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (140.91 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

MLS1547 fully antagonizes dopamine-mediated β-arrestin recruitment to the D2R in the DiscoveRx assay, with an IC50 of 9.9 μM. Similar results were obtained when MLS1547 was examined for antagonist activity in the D2R β-arrestin BRET assay, demonstrating an IC50 of 3.8 μM. MLS1547 is found to completely displace [3H]methylspiperone binding to the D2R, with a calculated Ki of 1.2 μM.

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