NP3-562 | NLRP3 inhibitor | Probechem Biochemicals

Chemical Structure : NP3-562

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NP3-562 (NP 3-562)

货号: 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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100 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	437.94
分子式	C19H24ClN5O3S
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-(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

参考文献

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

NP3-562 (NP 3-562)

生物&药学活性

物理化学性质&存储条件

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NP3-562 (NP 3-562)

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物理化学性质&存储条件

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