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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-CCR2-RA-[R]
CCR2-RA-[R]

Chemical Structure : CCR2-RA-[R]

CAS No.: 512177-83-2

CCR2-RA-[R] (CCR2-RA [R])

货号: PC-60323Not For Human Use, Lab Use Only.

CCR2-RA-[R] is a potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCR2-RA-[R] is a potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
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.
CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface.

物理化学性质&存储条件

分子量 351.802
分子式 C18H19ClFNO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one

参考文献

1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461.

2. Zweemer AJ, et al. Mol Pharmacol. 2013 Oct;84(4):551-61.

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