Chemical Structure : NP3-253
CAS No.:
2557349-50-3
NP3-253
Catalog No.: PC-23493Not For Human Use, Lab Use Only.
NP3-253 is a potent, selective and brain penetrant inhibitor of the NLRP3 inflammasome, inhibits IL-1β release in nigericin-stimulated THP-1 cells with IC50 of 0.5 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NP3-253 is a potent, selective and brain penetrant inhibitor of the NLRP3 inflammasome, inhibits IL-1β release in nigericin-stimulated THP-1 cells with IC50 of 0.5 nM.
NP3-253 inhibits IL-1β release from LPS/ATP-stimulated human whole blood with IC50 of 7 nM.
NP3-253 does not interfere with the NF-κB pathway (TNF-α > 100 μM) and did not inhibit either the NLRC4 or pyrin inflammasome (>33 μM).
NP3-253 shows good selectivity in an off-target panel of 29 enzymes, receptors, and ion channels tested up to 10 μM, with only some binding to the muscarinic receptor M2 (9.9 μM) and serotonin transporter 5HTT (3.8 μM).
NP3-253 (10 mg/kg, intraperitoneal (i.p.) injection) fully blocked IL-1β secretion in the peritoneum in C57BL/6JRj mice.
Physicochemical Properties
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M.Wt
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380.42
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Formula
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C19H23F3N4O
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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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(R)-2-(6-((1-Ethylpiperidin-3-yl)amino)pyridazin-3-yl)-3-methyl-5-(trifluoromethyl)phenol
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References
1. Mackay A, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c02350.
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