CCR2 antagonist 4
规格
Cas Number | 226226-39-7 |
规格或纯度 | 100% |
包装 | 5mg |
产品信息
品牌 | 阿拉丁 |
浓度 | 100% |
溶解性 | DMSO : ≥ 50 mg/mL (113.67 mM) |
过滤标签 | CCR,GPCR/G Protein,Immunology/Inflammation |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | CCR2拮抗剂4(帝人化合物1)是一种强效特异性CCR2拮抗剂,对CCR2b的IC 50 s为180 nM。CCR2 拮抗剂 4 能有效抑制 MCP-1 诱导的趋化作用,其 IC 50 为 24 nM。 |
英文描述 |
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC 50 s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC 50 of 24 nM In Vitro Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated CCR2 antagonist 4, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4. In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CCR2b 180 nM (IC 50 ) |