产品说明书

CCR2-RA-[R]

Print
Chemical Structure| 512177-83-2 同义名 : -
CAS号 : 512177-83-2
货号 : A316281
分子式 : C18H19ClFNO3
纯度 : 98%
分子量 : 351.8
MDL号 : MFCD11616183
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
实验方案
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
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.