[CAS NO. 315698-36-3] MLS1547
PRODUCTS SPECIFICATIONS [315698-36-3]
DESCRIPTION [315698-36-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 354.83 |
| Molecular Formula | C19H19ClN4O |
| SMILES | OC1=C2N=CC=CC2=C(Cl)C=C1CN3CCN(C4=NC=CC=C4)CC3 |
Summary
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist ( K i =1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling ( EC 50 =0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC 50 =9.9 μM) [1] [2] .
In Vitro
MLS1547 fully antagonizes dopamine-mediated β-arrestin recruitment to the D2R in the DiscoveRx assay, with an IC 50 of 9.9 μM. Similar results were obtained when MLS1547 was examined for antagonist activity in the D2R β-arrestin BRET assay, demonstrating an IC 50 of 3.8 μM. MLS1547 is found to completely displace [ 3 H]methylspiperone binding to the D2R, with a calculated K i of 1.2 μM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 93.93 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8183 mL | 14.0913 mL | 28.1825 mL |
| 5 mM | 0.5637 mL | 2.8183 mL | 5.6365 mL |
| 10 mM | 0.2818 mL | 1.4091 mL | 2.8183 mL |
References
- [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.