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.
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- Reinheit: 99.59%
- CAS. Nr.: 1345964-89-7
- Formel: C29H26BrN2PS
- Molecular Weight:545.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Biologische Aktivität
NPSR[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.0013 μM
Compound: 20e
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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
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[PMID: 24171469] |
| CHO | IC50 |
0.045 μM
Compound: 20e
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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
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[PMID: 24171469] |
| CHO | IC50 |
3.5 nM
Compound: 20e
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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
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[PMID: 24171469] |
| CHO | IC50 |
0.00096 μM
Compound: 20e
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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
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[PMID: 24171469] |
| CHO | IC50 |
0.96 nM
Compound: 20e
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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
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[PMID: 24171469] |
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.
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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.
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. Nr. 1345964-89-7
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Appearance Solid
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Molecular Weight 545.47
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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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)
Verweise
[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 |
ML154 Related Classifications
HY-108626 Related Classifications
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