CCR2-RA-[R]
规格
| Cas Number | 512177-83-2 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 37.5 mg/mL (106.59 mM; ultrasonic and warming and heat to 60°C) |
| 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-RA-[R] 是一种 C-C 趋化因子受体 2 型（CCR2）的异位拮抗剂，其 IC 50 为 103 nM。 |
| 英文描述 |
CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC 50 of 103 nM. In Vitro The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [ 125 I]CCL2 from CCR2 with an pIC 50 value of 6.1. The pK D of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CCR2 103 nM (IC 50 , in U2OS-CCR2 cells) |