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NP3-562

Chemical Structure : NP3-562

CAS No.: 2409825-32-5

NP3-562 (NP 3-562)

Catalog No.: PC-21638Not For Human Use, Lab Use Only.

NP3-562 is a potent, orally bioavailable NLRP3 inflammasome inhibitor, inhibits IL-1β in nigericin-stimulated THP-1 cells with IC50 of 90 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

NP3-562 is a potent, orally bioavailable NLRP3 inflammasome inhibitor, inhibits IL-1β in nigericin-stimulated THP-1 cells with IC50 of 90 nM.
NP3-562 potently inhibits IL-1β in human whole blood after LPS/ATP stimulation with IC50 of 214 nM, and IC50 of 248 nM for mouse whole blood stimulated with LPS/ATP.
NP3-562 binds to the NLRP3 NACHT domain with IC50 of 0.26 uM in FP binding assays, shows a unique binding mode as compared to the known sulfonylurea-based inhibitors.
NP3-562 (50 mg/kg po) caused 90% IL-1β inhibition at 1.68 ± 0.53 μM blood concentration in female C57BL/6 mice.
NP3-562 shows a clean off-target profile, including no mutagenic findings, no interference with the NF-κB pathway (TNFα IC50>100 μM).

Physicochemical Properties

M.Wt 437.94
Formula C19H24ClN5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-(2-Chloro-5-(2-hydroxypropan-2-yl)-8-oxothieno[2',3':4,5]pyrrolo[1,2-d][1,2,4]triazin-7(8H)-yl)-N-(1-methylpiperidin-3-yl)acetamide

References

1. Juraj Velcicky, et al. J Med Chem. 2024 Jan 4. doi: 10.1021/acs.jmedchem.3c02098.

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