CCR2 Covalent-IN-14

Chemical Structure : CCR2 Covalent-IN-14

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	590.413
分子式	C23H16Cl2F3N3O4S2
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	4-(4-Chloro-2-((4-chloro-3-(trifluoromethyl)phenyl)sulfonamido)phenoxy)-N-(2-thiocyanatoethyl)benzamide

参考文献

1. Ortiz Zacarías NV, et al. J Med Chem. 2021 Mar 11;64(5):2608-2621.