CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC 50 of 103 nM. In Vitro 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. CCR2-RA-[R] displaces [ 125 I]CCL2 from CCR2 with an pIC 50 value of 6.1. The pK D 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. 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”. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CCR2 103 nM (IC 50 , in U2OS-CCR2 cells)
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CCR2-RA-[R]
CAS number：512177-83-2 molecular formula：C18H19ClFNO3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 512177-83-2 | molecular formula | C18H19ClFNO3 |
| molecular weight | 351.8 g/mol | Exact mass | ≥98% |
| PSA | 57.600 Ų | logp | 4.300 |
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