Chemical Structure : NLRP3 inhibitor compound A
CAS No.:
2925431-13-4
NLRP3 inhibitor compound A
货号: PC-23598Not For Human Use, Lab Use Only.
NLRP3 inhibitor compound A is a potent, highly selective NLRP3 inflammasome inhibitor with IC50 of 67 nM for inhibition of IL-1β in PBMCs, targets ATPase activity of NLRP3 through binding to Walker A motif.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
NLRP3 inhibitor compound A is a potent, highly selective NLRP3 inflammasome inhibitor with IC50 of 67 nM for inhibition of IL-1β in PBMCs, targets ATPase activity of NLRP3 through binding to Walker A motif.
Compound A targets the same NACHT binding pocket as MCC950.
Compound A exhibits minimal effects on NLRC4, Pyrin, and AIM2 inflammasomes, shows no impact on IL-6 and TNF cytokine levels, and no cellular cytotoxicity in LPS-primed bone marrow-derived macrophages (BMDMs).
Compound A inhibited ASC speck formation in a dose–response manner in Nig-treated cells.
Compound A showed a 4.5-to-7-fold shift in potency with MWS mutant compared to WT BMDMs.
NLRP3 inhibitor compound A is a selective and potent NLRP3 inhibitor with improved activity compared to reference compound MCC950.
Compound A shows good potency and improved efficacy toward CAPS disease.
物理化学性质&存储条件
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分子量
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432.37
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分子式
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C18H15F3N8O2
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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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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N-([1,2,4]triazolo[4,3-b]pyridazin-6-yl)-2-(4-(dimethylamino)-1-oxo-6-(trifluoromethyl)phthalazin-2(1H)-yl)acetamide
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参考文献
1. Matico R, et al. MBO Mol Med. 2024 Dec 9. doi: 10.1038/s44321-024-00181-4.
