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CAS No.: 2165340-32-7

CU-CPT-9a Catalog No. CSN21261

Synonyms: CU-CPT-9a

CU-CPT9b is a selective inhibitor of TLR8 with IC50 and Kd of 0.7 nM and 21 nM.

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生物活性

实验方案

技术信息

生物活性

描述Toll-like receptor (TLR) family proteins play a crucial role in the initiation of the hosts' immune responses, which can trigger the proinflammatory signaling cascades that result in activation of nuclear factor (NF)-κB and upregulation of inflammatory cytokines and chemokines. This TLR response is crucial for helping to eliminate the pathogen and establishing long lasting adaptive responses, but also can cause various autoimmune diseases and inflammatory disorders^[1]. CU-CPT-9a is a specific TLR8 antagonist, with an IC₅₀ of 0.5 ± 0.1 nM. The elevation of the downstream protein levels induced by R848 in both THP-1 and HEK-Blue TLR8 cells can be reversed by CU-CPT-9a in a dose-dependent manner. Immunoblot analysis results support the notion that the inhibitory effects of CU-CPT-9a occur specifically through TLR8 in cells. Moreover, CU-CPT-9a significantly suppresses the TNF-α level in a dose-dependent manner^[1]. Results of this proof-of-concept study show that CU-CPT-9a treatment exerts potent anti-inflammatory effects in the specimens of OA (osteoarthritis), RA (rheumatoid arthritis), and AOSD (adult-onset Still's disease) patients^[1].
参考文献

[1] Zhang S, Hu Z, Tanji H, Jiang S, Das N, Li J, Sakaniwa K, Jin J, Bian Y, Ohto U, Shimizu T, Yin H. Small-molecule inhibition of TLR8 through stabilization of its resting state. Nat Chem Biol. 2018 Jan;14(1):58-64. doi: 10.1038/nchembio.2518. Epub 2017 Nov 20. PMID: 29155428; PMCID: PMC5726935.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7692 mL
- 18.8459 mL
- 37.6918 mL
- 5 mM
- 0.7538 mL
- 3.7692 mL
- 7.5384 mL
- 10 mM
- 0.3769 mL
- 1.8846 mL
- 3.7692 mL

技术信息

CAS号

2165340-32-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15NO2

运输

蓝冰

分子量

265.31

别名

CU-CPT-9a

溶解度

DMSO	115.0 mg/mL (433.5 mM)
Water	insoluble

动物实验配方

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