CCR2 Antagonist (CAS 445479-97-0)
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CCR2 Antagonist is a cell-permeable cis-diamidocyclohexyl urea compound with high affinity binding to CKR-2B (chemokine (C-C motif) receptor 2 CCR2), also known as CD192 (cluster of differentiation 192). CKR-2B is a G protein-coupled receptor with a unique conserved glutamic acid residue in transmembrane 7, Glu291. Research shows that this conserved residue is a critical site for small molecule antagonist binding. MCP-1 (chemokine (C-C motif) ligand 2 CCL2) is a specific chemokine for the CKR-2B receptor and is responsible for recruiting monocytes, memory T cells, and dendritic cells to sites of tissue injury and infection. CCR2 Antagonist displays high affinity binding for CKR-2B (IC50 = 5.1 nM) and potent functional antagonism (calcium flux IC50 = 18 nM and chemotaxis IC 50 = 1 nM). Although Glu291 is a key receptor residue for CKR-2B, CCR2 Antagonist studies show that this inhibitor is not reliant upon Glu291 for its affinity binding, rather a nearby site. CCR2 Antagonist exhibits preferential binding for CKR-2B over CKR-3 (CCR3).
CCR2 Antagonist (CAS 445479-97-0) References
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Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CCR2 Antagonist, 5 mg | sc-202525 | 5 mg | $299.00 |