Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCR2-RA-[R] 是一种 C-C 趋化因子受体 2 型 (CCR2) 变构拮抗剂,IC50值为103 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 443 | 现货 | ||
5 mg | ¥ 721 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 786 | 现货 |
产品描述 | CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM). |
靶点活性 | CCR2:103 nM (in U2OS-CCR2 cells) |
体外活性 | CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively[2]. 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. 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”[3]. |
别名 | (5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮 |
分子量 | 351.8 |
分子式 | C18H19ClFNO3 |
CAS No. | 512177-83-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 125 mg/mL (355.32 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8425 mL | 14.2126 mL | 28.4252 mL | 71.0631 mL |
5 mM | 0.5685 mL | 2.8425 mL | 5.685 mL | 14.2126 mL | |
10 mM | 0.2843 mL | 1.4213 mL | 2.8425 mL | 7.1063 mL | |
20 mM | 0.1421 mL | 0.7106 mL | 1.4213 mL | 3.5532 mL | |
50 mM | 0.0569 mL | 0.2843 mL | 0.5685 mL | 1.4213 mL | |
100 mM | 0.0284 mL | 0.1421 mL | 0.2843 mL | 0.7106 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CCR2-RA-[R] 512177-83-2 Immunology/Inflammation Microbiology/Virology CCR Inhibitor inhibit CCR-2-RA-[R] CC chemokine receptor CCR2RA[R] (5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮 CCR2 RA [R] inhibitor