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
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M.Wt
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437.94
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Formula
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C19H24ClN5O3S
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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-(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
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References
1. Juraj Velcicky, et al. J Med Chem. 2024 Jan 4. doi: 10.1021/acs.jmedchem.3c02098.
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