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Chemical Structure : CCR2 Covalent-IN-14
Catalog No.: PC-72895Not For Human Use, Lab Use Only.
CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.
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CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.
CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).
CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.
The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2.
| M.Wt | 590.413 | |
| Formula | C23H16Cl2F3N3O4S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ortiz Zacarías NV, et al. J Med Chem. 2021 Mar 11;64(5):2608-2621.
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