2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. ML154

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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ML154 Chemical Structure

ML154 Chemical Structure

CAS No. : 1345964-89-7

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target

NPSR[1]
Cellular Effect
Cell Line Type Value Description References
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
0.0013 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]
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.

ML154 Related Antibodies

Western Blot Analysis[1]

Cell Line: CHO cells expressing NPSR
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 30 min
Result: Exhibited the most potent inhibition on NPS-induced ERK phosphorylation.
In Vivo

ML154 (NCGC84; 1 mg/kg; i.p; once) blocks alcohol-induced ERK-phosphorylation in the rat central amygdala, a region involved in regulation of alcohol intake. ML154 also decreases operant alcohol self-administration, and lowers motivation for alcohol reward as measured using progressive ratio responding[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (300-350 g) injected with alcohol[1]
Dosage: 1 mg/kg (10% Solutol, 10% N,N-dimethylacetamide, and 80% 10 mM PBS, pH 7.4)
Administration: Intraperitoneal injection; once
Result: Inhibited alcohol-induced central ERK phosphorylation in vivo.
Molecular Weight

545.47

Formula

C29H26BrN2PS
CAS No.
Appearance

Solid

Color

White to off-white

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8333 mL 9.1664 mL 18.3328 mL
5 mM 0.3667 mL 1.8333 mL 3.6666 mL
View the 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.

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Purity & Documentation
References

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
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ML154 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML1541345964-89-7NCGC84ML 154ML-154NCGC 84NCGC-84Neuropeptide Y ReceptorNPY receptorNPSRanxietyaddictionfood disorderInhibitorinhibitorinhibit

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