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首页-小分子抑制剂&激动剂-Immunology/Inflammation-NOD-like Receptor (NLR)-NLRP3 inhibitor NIC-11
NLRP3 inhibitor NIC-11

Chemical Structure : NLRP3 inhibitor NIC-11

CAS No.: 2409824-75-3

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NLRP3 inhibitor NIC-11 (NIC-11)

货号: PC-22042Not For Human Use, Lab Use Only.

NIC-11 is a highly potent broad-spectrum NLRP3 inhibitor, inhibits NLRP3 inflammasome activation (IL-1β release) in mouse macrophages with IC50 of 69 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NIC-11 is a highly potent broad-spectrum NLRP3 inhibitor, inhibits NLRP3 inflammasome activation (IL-1β release) in mouse macrophages with IC50 of 69 nM.
NIC-11 dose-dependently inhibited LDH release in mouse BMDMs.
NIC-11 targets NLRP3 signaling upstream of caspase-1 in mouse BMDMs, does not target NLRP3 priming.
NIC-11 suppresses LPS-induced NLRP3 activation downstream of TLR4-induced NF-κB signaling, also blocks the activation of the NLRP3 inflammasome by the endogenous STING agonist cGAMP in primary human monocytes.
NIC-11 shows potent activity in LPS-stimulated blood monocytes and dose-dependently inhibited IL-1ß secretion with IC50 of 16 nM in primary human monocytes.
NIC-11 shows direct binding to the NLRP3 NACHT domain with IC50 of 212 nM in NanoBRET target engagement assays.
NIC-11 inhibits pyroptosis of MWS-associated Nlrp3A350V BMDMs.
NIC-11(50 mg/kg) selectively reduces circulating IL-1ß levels in the LPS-endotoxemia model in mice and inhibits NLRP3 inflammasome activation in CAPS patient monocytes and mouse macrophages.

物理化学性质&存储条件

分子量 418.86
分子式 C17H15ClN6O3S
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

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-(pyrimidin-4-yl)acetamide

参考文献

1. Lieselotte Vande Walle, et al. Life Sci Alliance. 2024 Mar 22;7(6):e202402644.

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