Chemical Structure : CCR2-RA-[R]
CAS No.:
512177-83-2
CCR2-RA-[R]
(CCR2-RA [R])
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
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Biological Activity
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.
Physicochemical Properties
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M.Wt
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351.802
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Formula
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C18H19ClFNO3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
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References
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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![CCR2-RA-[R]](userfiles/product/PC-60323.gif)
