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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Interleukin Receptor-AIK3a305
AIK3a305

Chemical Structure : AIK3a305

CAS No.: 2419902-92-2

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AIK3a305 (AIK3-305)

货号: PC-26254Not For Human Use, Lab Use Only.

AIK3a305 (AIK3-305) is an allosteric inhibitor of Jmitogen-activated protein kinases (MAPK), particularly JNK, and a potent and selective, orally available inhibitor IL-1β release in human monocyte-derived macrophages with IC50 of 28 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AIK3a305 (AIK3-305) is an allosteric inhibitor of Jmitogen-activated protein kinases (MAPK), particularly JNK, and a potent and selective, orally available inhibitor IL-1β release in human monocyte-derived macrophages with IC50 of 28 nM.
AIK3a305 does not interfere expression levels of IL-1α, IL-2, IL-6, IL-8 or GM-CSF.
AIK3a305 shows direct biophysical interactions to p38α MAPK with SPR KD of 12 nM.
AIK3a305 (10-20 mg/kg) inhibits IL-1β secretion in LPS endotoxic shock model in male BALB/c mice.
AIK3a305 selectively inhibited LPS- and palmitate-induced IL1β expression in macrophages, while protecting hepatocytes from intracellular lipid accumulation and lipoapoptosis.
AIK3a305 attenuated disease progression in animals fed either a HFD or a CDAA diet, as evidenced by improved liver histopathology, including reduced steatosis and inflammation, in preclinical models of MASLD.

物理化学性质&存储条件

分子量 532.05
分子式 C26H30ClN3O5S
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

6-(4-(4-chlorophenoxy)piperidin-1-yl)-5-(4-ethoxyphenoxy)-N,N-dimethylpyridine-3-sulfonamide

参考文献

1. Berlana Á, et al. Biomed Pharmacother. 2026 Feb;195:119052.

2. Zegarra-Valdivia JA, et al. Geroscience. 2022 Aug;44(4):2243-2257.

3. Carrasco E, et al. Eur J Med Chem. 2021 Nov 5;223:113620.

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