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ML154

Chemical Structure : ML154

CAS No.: 1345964-89-7

ML154 (ML-154, NCGC84, NCGC00185684)

Catalog No.: PC-61554Not For Human Use, Lab Use Only.

ML154 (NCGC00185684) is a potent, selective, brain penetrant NPSR (Neuropeptide S receptor, GPR154) antagonist with IC50 of 22.1 nM and 36.5 nM in Ca2+ assay and cAMP assay, respectively.

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Biological Activity

ML154 (NCGC00185684) is a potent, selective, brain penetrant NPSR (Neuropeptide S receptor, GPR154) antagonist with IC50 of 22.1 nM and 36.5 nM in Ca2+ assay and cAMP assay, respectively.
ML154 shows biased antagonist properties, and preferentially blocks ERK-phosphorylation over intracellular cAMP or calcium responses to NPS in vitro.
ML154 blocks alcohol-induced ERK-phosphorylation in the rat central amygdala, also decreases operant alcohol self-administration, and lowers motivation for alcohol reward in rats.

Physicochemical Properties

M.Wt 545.47
Formula C29H26N2PS.Br
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-cinnamyl-3-(diphenylphosphorothioyl)-2-methyl-2,3-dihydroimidazo[1,2-a]pyridin-1-ium

References

1. Thorsell A, et al. J Neurosci. 2013 Jun 12;33(24):10132-42.

2. Patnaik S, et al. Probe Reports from the NIH Molecular Libraries Program [Internet].

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