ML154
Based on 1 Customer Validation
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively.
For research use only. We do not sell to patients.
- Purity : 99.59%
- CAS No.: 1345964-89-7
- Formula: C29H26BrN2PS
- Molecular Weight:545.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
NPSR[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.0013 μM
Compound: 20e
|
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay
|
[PMID: 24171469] |
| CHO | IC50 |
0.045 μM
Compound: 20e
|
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay
|
[PMID: 24171469] |
| CHO | IC50 |
3.5 nM
Compound: 20e
|
Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting
Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting
|
[PMID: 24171469] |
| CHO | IC50 |
0.00096 μM
Compound: 20e
|
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
|
[PMID: 24171469] |
| CHO | IC50 |
0.96 nM
Compound: 20e
|
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
|
[PMID: 24171469] |
In Vitro
ML154 (NCGC84; 0.001-1 μM; 30 min ) inhibits NPS-induced ERK phosphorylation in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:CHO cells expressing NPSR
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM
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Incubation Time:30 min
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Result:Exhibited the most potent inhibition on NPS-induced ERK phosphorylation.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (300-350 g) injected with alcohol[1]
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Dosage:1 mg/kg (10% Solutol, 10% N,N-dimethylacetamide, and 80% 10 mM PBS, pH 7.4)
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Administration:Intraperitoneal injection; once
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Result:Inhibited alcohol-induced central ERK phosphorylation in vivo.
Chemical Information
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CAS No. 1345964-89-7
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Appearance Solid
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Molecular Weight 545.47
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Formula C29H26BrN2PS
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Color White to off-white
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SMILES
S=P(C1=CC=CC=C1)(C2=CC=CC=C2)C3=C(C)[N+](C/C=C/C4=CC=CC=C4)=C5N3C=CC=C5.[Br-]
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Synonyms
NCGC84
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 62.5 mg/mL (114.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Annika Thorsell, et al. 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. 2013 Jun 12;33(24):10132-42. [Content Brief]
[2]. İrem Akçalı, et al. The regulatory role of central neuropeptide-S in locomotion. Peptides. 2023 Dec:170:171110. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8333 mL | 9.1664 mL | 18.3328 mL | 45.8320 mL |
| 5 mM | 0.3667 mL | 1.8333 mL | 3.6666 mL | 9.1664 mL | |
| 10 mM | 0.1833 mL | 0.9166 mL | 1.8333 mL | 4.5832 mL | |
| 15 mM | 0.1222 mL | 0.6111 mL | 1.2222 mL | 3.0555 mL | |
| 20 mM | 0.0917 mL | 0.4583 mL | 0.9166 mL | 2.2916 mL | |
| 25 mM | 0.0733 mL | 0.3667 mL | 0.7333 mL | 1.8333 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6111 mL | 1.5277 mL | |
| 40 mM | 0.0458 mL | 0.2292 mL | 0.4583 mL | 1.1458 mL | |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3667 mL | 0.9166 mL | |
| 60 mM | 0.0306 mL | 0.1528 mL | 0.3055 mL | 0.7639 mL | |
| 80 mM | 0.0229 mL | 0.1146 mL | 0.2292 mL | 0.5729 mL | |
| 100 mM | 0.0183 mL | 0.0917 mL | 0.1833 mL | 0.4583 mL |