CCR2 Covalent-IN-14
Modify Date: 2024-01-14 15:32:07
CCR2 Covalent-IN-14 structure
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Common Name | CCR2 Covalent-IN-14 | ||
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| CAS Number | 2714478-83-6 | Molecular Weight | 590.413 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H16Cl2F3N3O4S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CCR2 Covalent-IN-14CCR2 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. |
| Name | CCR2 Covalent-IN-14 |
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| Description | 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. |
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| References | 1. Ortiz Zacarías NV, et al. J Med Chem. 2021 Mar 11;64(5):2608-2621. |
| Molecular Formula | C23H16Cl2F3N3O4S2 |
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| Molecular Weight | 590.413 |