ML 154

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Cat.No. 5161 - ML 154 | C29H26N2PS.Br | CAS No. 1345964-89-7
Description: Potent Neuropeptide S receptor antagonist
Chemical Name: 3-(Diphenylphosphinothioyl)-2-methyl-1-[(2E)-3-phenyl-2-propen-1-yl]imidazo[1,2-a]pyridinium bromide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent neuropeptide S receptor (NPSR) antagonist (pA2 = 9.98). Inhibits neuropeptide S-induced ERK phosphorylation over cAMP responses and calcium responses (IC50 values are 9.3, 22.1 and 36.5 nM, respectively). Appears to modulate addictive behavior in vivo. Displays no activity against vasopressin V1B receptors. Brain penetrant.

Technical Data

M. Wt 545.47
Formula C29H26N2PS.Br
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1345964-89-7
PubChem ID 46930969
InChI Key CJAQCMBWGUOBIX-ZUQRMPMESA-M
Smiles CC1=C(P(C4=CC=CC=C4)(C5=CC=CC=C5)=S)N3C(C=CC=C3)=[N+]1C/C=C/C2=CC=CC=C2.[Br-]

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.55 100
ethanol 27.27 50

Preparing Stock Solutions

The following data is based on the product molecular weight 545.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.17 mL 18.33 mL
5 mM 0.37 mL 1.83 mL 3.67 mL
10 mM 0.18 mL 0.92 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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References

References are publications that support the biological activity of the product.

Patnaik et al (2013) Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor. J Med Chem. 56 9045 PMID: 24171469

Thorsell et al (2013) A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats. J.Neurosci. 33 10132 PMID: 23761908


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