中文名 | CPD1578 |
英文名 | CU-CPT-8m |
别名 | 化合物CU-CPT-8M 7-(间甲苯基)吡唑并[1,5-A]嘧啶-3-甲酰胺 |
英文别名 | CPD1578 CU-CPT-8m CU-CPT-8M TLR8 INHIBITOR TLR8-specific antagonist 7-(m-tolyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 7-(3-methylphenyl)- |
CAS | 125079-83-6 |
化学式 | C14H12N4O |
分子量 | 252.27 |
密度 | 1.35±0.1 g/cm3(Predicted) |
酸度系数 | 12.41±0.50(Predicted) |
存储条件 | Sealed in dry,Room Temperature |
体外研究 | CU-CPT-8m is a specific TLR8 antagonist, with an IC 50 of 67±10 nM and negligible cytotoxicity. The K d value of CU-CPT-8m is determined to be 220 nM. CU-CPT-8m only reduces the proinflammatory response in the TLR8-overexpressing cells strongly supports that CU-CPT-8m directly recognizes TLR8 in cells. It is particularly notable that TLR7 signaling is not affected at concentrations up to 75 μM. TLR7 and TLR8 are closely related and share many common ligands. Treatment of 1 μM CU-CPT-8m completely abolishes the elevation of TNF-α and IL-8 mRNA levels induced by R848. CU-CPT-8m inhibits R848-induced TNF-α production in the differentiated THP-1 monocytes cells in a dose-dependent manner with an IC 50 of 90±10 nM, which is in good agreement with its IC 50 value determined in HEK-Blue TLR8 cells. |
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