货号 | 11479-1mg |
描述 | Monocyte chemoattractant protein-1 (MCP-1/CCL2) and other members of the MCP cluster (MCP-2/CCL8 and MCP-3/CCL7) are potent chemotactic cytokines that collaboratively promote inflammation through monocyte-macrophage recruitment. Bindarit is an indazolic derivative that inhibits the expression of CCL2, CCL7, and CCL8, as well as IL-12.1 It can inhibit LPS- or C. albicans-induced production of CCL2 in human monocytes with IC50 values of 172 and 403 µM, respectively.1,2 Bindarit has been shown to downregulate the NF-κB pathway, preventing p65 and p65/p50-mediated CCL2 promoter activation.1 Through potent suppression of CCL2 transcription, bindarit has been reported to reduce symptoms in several animal models of human inflammatory diseases, including lupus nephritis, arthritis, cancer, and encephalomyelitis.1,3,4,5 |
别名 | AF 2838; |
供应商 | Cayman |
应用文献 | |
1.Mora, E.,Guglielmotti, A.,Biondi, G., et al. Bindarit: An anti-inflammatory small molecule that modulates the NFκB pathway. Cell Cycle 11(1), 159-169 (2016). 2.Sironi, M.,Guglielmotti, A.,Polentarutti, N., et al. A small synthetic molecule capable of preferentially inhibiting the production of the CC chemokine monocyte chemotactic protein-1. European Cytokine Network 10(3), 437-442 (1999). 3.Zoja, C.,Corna, D.,Benedetti, G., et al. Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney International 53(3), 726-734 (1998). 4.Chen, W.,Foo, S.S.,Taylor, A., et al. Bindarit, an inhibitor of monocyte chemotactic protein synthesis, protects against bone loss induced by chikungunya virus infection. Journal of Virology 89(1), 581-593 (2015). 5.Ge, S.,Shrestha, B.,Paul, D., et al. The CCL2 synthesis inhibitor bindarit targets cells of the neurovascular unit, and suppresses experimental autoimmune encephalomyelitis. Journal of Neuroinflammation 9:171, (2012). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 324.4 |
分子式 | C19H20N2O3 |
CAS号 | 130641-38-2 |
稳定性 | ≥ 2 years |
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