An agonist of dopamine D2 receptors
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MLS-1547

Item No. 27648

Technical Information
Formal Name
5-chloro-7-[[4-(2-pyridinyl)-1-piperazinyl]methyl]-8-quinolinol
CAS Number
315698-36-3
Molecular Formula
C19H19ClN4O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:9): 0.1 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
251, 309 nm
SMILES
OC1=C(C=C(Cl)C2=C1N=CC=C2)CN(CC3)CCN3C4=CC=CC=N4
InChi Code
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
InChi Key
OPEJNANYABTIGC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MLS-1547 is a G protein-biased agonist of dopamine D2 receptors (EC50 = 0.37 μM in a calcium mobilization assay).1 It inhibits forskolin-induced cAMP accumulation in CHO cells expressing human D2 receptors (EC50 = 0.26 μM) but is inactive in β-arrestin recruitment assays. MLS-1547 antagonizes dopamine-induced β-arrestin recruitment in cell-based assays with IC50 values ranging from 3.8 to 9.9 μM.1 It is also an inhibitor of type II secretion in Gram-negative bacteria.2 MLS-1547 inhibits secretion of phospholipase C (PlcH/N) and the virulence factor elastase (LasB) from P. aeruginosa (IC50s = 15 and 13 μM, respectively) and inhibits B. pseudomallei protease secretion by 90.8% when used at a concentration of 25 μM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Free, R.B., Chun, L.S., Moritz, A.E., et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol. Pharmacol. 86(1), 96-105 (2014).

    2. Moir, D.T., Di, M., Wong, E., et al. Development and application of a cellular, gain-of-signal, bioluminescent reporter screen for inhibitors of type II secretion in Pseudomonas aeruginosa and Burkholderia pseudomallei. J. Biomol. Screen. 16(7), 694-705 (2011).