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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: ML 154, supplier, ML154, Potent, selective, Neuropeptide, S, receptors, NPSR, antagonists, ERK, phosphorylation, additive, behaviour, Blood, brain, barrier, permeable, Other, Peptide, Receptors, Other, Peptide, Receptors, Tocris Bioscience
