NP3-253

Chemical Structure : NP3-253

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	380.42
分子式	C19H23F3N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-2-(6-((1-Ethylpiperidin-3-yl)amino)pyridazin-3-yl)-3-methyl-5-(trifluoromethyl)phenol

参考文献

1. Mackay A, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c02350.

NP3-253

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物理化学性质&存储条件

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NP3-253

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