Chemical Structure : NPSR1 antagonist Compound 6
CAS No.:
3113770-74-1
NPSR1 antagonist Compound 6
Catalog No.: PC-28044Not For Human Use, Lab Use Only.
NPSR1 antagonist Compound 6 is a potent, selective and peripherally biased neuropeptide S receptor 1 (NPSR1, GPR154) with IC50 of 0.35 nM and 0.15 nM in calcium assay against NPSR1-A and NPSR1-B, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NPSR1 antagonist Compound 6 is a potent, selective and peripherally biased neuropeptide S receptor 1 (NPSR1, GPR154) with IC50 of 0.35 nM and 0.15 nM in calcium assay against NPSR1-A and NPSR1-B, respectively.
NPSR1 antagonist Compound 6 has IC50 of 0.22 nM in the cAMP assay.
NPSR1 antagonist Compound 6 effectively inhibits the expression of the NPS-induced markers without affecting expression of non-NPS induced genes in NPSR1-A expressing fibroblasts.
NPSR1 antagonist Compound 6 (10 mg/kg) reduces TNF-α and altered macrophage populations in zymosan-induced inflammatory mouse model.
Physicochemical Properties
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M.Wt
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528.69
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Formula
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C30H42F2N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-((4,4-difluoro-1-(4-methylpiperazin-1-yl)cyclohexyl)methyl)-N-((1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)cyclohexanecarboxamide
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References
1. Berger KJ, et al. Bioorg Med Chem Lett. 2025 Dec 1;128:130353.
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