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CU-CPT-9a

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Chemical Structure| 2165340-32-7 同义名 : -
CAS号 : 2165340-32-7
货号 : A624532
分子式 : C17H15NO2
纯度 : 98%
分子量 : 265.307
MDL号 : MFCD31689252
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 130 mg/mL(490 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.77mL

0.75mL

0.38mL

18.85mL

3.77mL

1.88mL

37.69mL

7.54mL

3.77mL

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.