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CCR2-RA-[R]

货号:A316281

CCR2-RA-[R]是一种变构拮抗剂,特异性抑制 C-C 趋化因子受体2 (CCR2),其 IC50 为 103 nM,具有潜在的抗炎抗肿瘤活性。

CCR2-RA-[R] 化学结构 CAS号:512177-83-2
CCR2-RA-[R] 化学结构
CAS号:512177-83-2
CCR2-RA-[R] 3D分子结构
CAS号:512177-83-2
CCR2-RA-[R] 化学结构 CAS号:512177-83-2
CCR2-RA-[R] 3D分子结构 CAS号:512177-83-2
规格 价格 库存 数量
50μL*10mM(DMSO) ¥119随货¥89 咨询
100μL*10mM(DMSO) ¥169随货¥119 咨询
250μL*10mM(DMSO) ¥299随货¥209 咨询
500μL*10mM(DMSO) ¥429随货¥309 咨询
10mM*1mL(DMSO) ¥678 咨询
5mg ¥554 咨询
10mg ¥882 咨询
25mg ¥1764 咨询
50mg ¥3024 咨询
100mg ¥4788 咨询
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CCR2-RA-[R] 纯度/质量文件 产品仅供科研

货号:A316281 标准纯度:
批次查询: 批次纯度:

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产品名称 CCR 其他靶点 纯度
Maraviroc ++

MIP-1α, IC50: 3.3 nM

MIP-1β, IC50: 5.2 nM

99%+
DAPTA +++

CM235-CCR5, IC50: 0.32 nM

gp120 Bal-CCR5, IC50: 0.06 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CCR2-RA-[R] 生物活性

描述 The chemokine receptor CCR2, a G protein-coupled receptor implicated in numerous chronic inflammatory diseases, has led to the development of various small molecule antagonists. CCR2-RA-[R] effectively displaces [125I]CCL2 from CCR2 with a pIC50 value of 6.1, while its pKD for CCR2 and CCR5 are 8.8±0.1 and 7.0±0.1 respectively[2]. CCR2-RA-[R] inhibits CCR2 non-competitively by preventing activation-associated conformational changes and the formation of the G protein-binding interface. The drug-binding pocket of CCR2-RA-[R] is notably enclosed and features a beneficial mix of hydrophobic and polar characteristics that enhance its "druggability"[3].
体外研究

The chemokine receptor CCR2, a G protein-coupled receptor implicated in numerous chronic inflammatory diseases, has led to the development of various small molecule antagonists. CCR2-RA-[R] effectively displaces [125I]CCL2 from CCR2 with a pIC50 value of 6.1, while its pKD for CCR2 and CCR5 are 8.8±0.1 and 7.0±0.1 respectively[2].

CCR2-RA-[R] inhibits CCR2 non-competitively by preventing activation-associated conformational changes and the formation of the G protein-binding interface. The drug-binding pocket of CCR2-RA-[R] is notably enclosed and features a beneficial mix of hydrophobic and polar characteristics that enhance its "druggability"[3].

CCR2-RA-[R] 参考文献

[1]Zweemer AJ, et al. Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2. Mol Pharmacol. 2014 Oct;86(4):358-68.

[2]Zheng Y, et al. Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists. Nature. 2016 Dec 15;540(7633):458-461.

CCR2-RA-[R] 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.21mL

2.84mL

1.42mL

28.43mL

5.69mL

2.84mL

CCR2-RA-[R] 技术信息

CAS号512177-83-2
分子式C18H19ClFNO3
分子量 351.8
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 35 mg/mL(99.49 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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