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CAS No.: 125079-83-6

CU-CPT-8m Catalog No. CSN21226

Synonyms: TLR8-specific antagonist

CU-CPT8m is a Toll-like receptor 8 (TLR8) specific small-molecule inhibitor that exerts “potent anti-inflammatory effects” on the tissue of patients with arthritis.

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技术信息

生物活性

描述Endosomal Toll-like receptors are highly analogous sensors for various viral or bacterial RNA and DNA molecular patterns. CU-CPT8m is a specific TLR8 antagonist, with an IC₅₀ of 67±10 nM and K_d of 220 nM. In HEK-Blue cells overexpressing each individual TLR, CU-CPT8m (1 μM) only reduces the proinflammatory response in the TLR8-overexpressing ones supporting that CU-CPT8m selectively inhibits TLR8 signaling. Treatment of 1 μM CU-CPT8m completely abolished the elevation of various cytokines both on the mRNA levels and protein levels induced by R848. In the synovial cells from synovial tissue of osteoarthritis (OA) patients, 24 h treatment of CU-CPT8m represented that it exerted significant inhibitory effects in suppressing the spontaneous release of TNF-α and IL-1β (key cytokines in the process of chronic joint inflammation) from synovial membrane cultures with little cytotoxicity up to 100 μM ^[1].
作用机制CU-CPT8m is sandwiched between two protomers (TLR8 and TLR8*, asterisks are used to indicate the second TLR8 and its residues) and is accommodated in a hydrophobic pocket on the protein-protein interface of TLR8 and TLR8* .
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
- 3.9640 mL
- 19.8199 mL
- 39.6399 mL
- 5 mM
- 0.7928 mL
- 3.9640 mL
- 7.9280 mL
- 10 mM
- 0.3964 mL
- 1.9820 mL
- 3.9640 mL

技术信息

CAS号

125079-83-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H12N4O

运输

蓝冰

分子量

252.27

别名

TLR8-specific antagonist

溶解度

DMSO	30.0 mg/mL (118.9 mM) warming

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