Name | CCR2 Covalent-IN-14 | CAS# | 2714478-83-6 | |
---|---|---|---|---|
Price | $Inquiry/100mg $Inquiry/250mg $Inquiry/1g | Purity | 98.0% | |
Stocking Period |
3 Day | Stock | 3 | |
Product Webpage: | https://www.dcchemicals.com/product_show-ccr2covalent-in-14.html |
Detail
Product Information
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. |