CCR2
CCR2 is a CC chemokine receptor that mediates MCP-1/CCL2-dependent monocyte chemotaxis, receptor binding, and ligand internalization in inflammatory and vascular contexts[1][2]. Mechanistically, the CCR2 amino-terminal domain is necessary and sufficient for high-affinity MCP-1 binding, while tyrosine sulfation enhances CCR2 interaction with monomeric and dimeric MCP-1 and supports leukocyte recruitment[1][3]. In human monocytes, LDL increases CCR2 expression and strengthens MCP-1 chemotactic responses, linking CCR2 signaling to monocyte recruitment during atherogenesis[4]. In disease models, leukocyte-derived CCR2 is critical for angiotensin II-accelerated atherosclerosis and aneurysm formation in hypercholesterolemic mice[5]. CCR2 also mediates MCP-1 binding and internalization along brain microvessels, supporting its use in blood-brain barrier and neuroinflammation models[6]. Compared with related isoforms, CCR2A and CCR2B show cell-specific distribution in idiopathic inflammatory myopathies, where CCR2A appears in vessel walls and mononuclear cells, while CCR2B appears in satellite cells, neuromuscular junction domains, and regenerative fibers[7]. For experimental applications, MCP-1 binds and activates CCR2B as a monomer, and CCR2-blocking antibodies reduce myeloma-cell migration toward bone marrow stromal chemokines[8][9].
References:
- [1]. Monteclaro FS, et al. The amino-terminal domain of CCR2 is both necessary and sufficient for high affinity binding of monocyte chemoattractant protein 1. Receptor activation by a pseudo-tethered ligand. J Biol Chem. 1997 Sep 12;272(37):23186-90. [Content Brief]
- [2]. Preobrazhensky AA, et al. Monocyte chemotactic protein-1 receptor CCR2B is a glycoprotein that has tyrosine sulfation in a conserved extracellular N-terminal region. J Immunol. 2000 Nov 1;165(9):5295-303. [Content Brief]
- [3]. Tan JHY, et al. Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1). J Biol Chem. 2013 Apr 5;288(14):10024-10034. [Content Brief]
- [4]. Han KH, et al. Chemokine receptor CCR2 expression and monocyte chemoattractant protein-1-mediated chemotaxis in human monocytes. A regulatory role for plasma LDL. Arterioscler Thromb Vasc Biol. 1998 Dec;18(12):1983-91. [Content Brief]
- [5]. Ishibashi M, et al. Bone marrow-derived monocyte chemoattractant protein-1 receptor CCR2 is critical in angiotensin II-induced acceleration of atherosclerosis and aneurysm formation in hypercholesterolemic mice. Arterioscler Thromb Vasc Biol. 2004 Nov;24(11):e174-8. [Content Brief]
- [6]. Dzenko KA, et al. The chemokine receptor CCR2 mediates the binding and internalization of monocyte chemoattractant protein-1 along brain microvessels. J Neurosci. 2001 Dec 1;21(23):9214-23. [Content Brief]
- [7]. Bartoli C, et al. CCR2A and CCR2B, the two isoforms of the monocyte chemoattractant protein-1 receptor are up-regulated and expressed by different cell subsets in idiopathic inflammatory myopathies. Acta Neuropathol. 2001 Oct;102(4):385-92. [Content Brief]
- [8]. Paavola CD, et al. Monomeric monocyte chemoattractant protein-1 (MCP-1) binds and activates the MCP-1 receptor CCR2B. J Biol Chem. 1998 Dec 11;273(50):33157-65. [Content Brief]
- [9]. Vande Broek I, et al. Chemokine receptor CCR2 is expressed by human multiple myeloma cells and mediates migration to bone marrow stromal cell-produced monocyte chemotactic proteins MCP-1, -2 and -3. Br J Cancer. 2003 Mar 24;88(6):855-62. [Content Brief]
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CCR2 Related Products (53)
Related Products (53)
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Recombinant Proteins (3)
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Antibodies (1)
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AZD2423
0 ImagesAZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux .
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CCR2-IN-1
0 ImagesCat. No.: HY-402739CAS No.: 3088041-47-5CCR2-IN-1 (Compound HO11553-TM) is a G protein-coupled receptor CCR2 inhibitor. CCR2-IN-1 slows the progression of idiopathic pulmonary fibrosis. CCR2-IN-1 can be used for the research of idiopathic pulmonary fibrosis.
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PF-04634817 succinate
0 ImagesPF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
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CCR2 antagonist 1
0 ImagesCCR2 antagonist 1 (compound 15a) is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM.
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JNJ-41443532
0 ImagesSynonyms: CCR2 antagonist 5JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease.
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JNJ-27141491
0 ImagesCat. No.: HY-110132CAS No.: 871313-59-6JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2.
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PF-04634817
0 ImagesCat. No.: HY-117621CAS No.: 1228111-63-4
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INCB3344 R-isomer
0 ImagesCat. No.: HY-50674APurity: 98.01%INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
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INCB 3284 dimesylate
0 ImagesCat. No.: HY-15450CAS No.: 887401-93-6INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
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YJC-10592
0 ImagesCat. No.: HY-136768CAS No.: 1226894-87-6YJC-10592 is an orally active CCR-2 antagonist. YJC-10592 binds to HAS. YJC-10592 can be used in the research of asthma and idiopathic dermatitis.
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JNJ-17166864
0 ImagesCat. No.: HY-129991CAS No.: 874887-03-3JNJ-17166864 is a highly selective CCR2 antagonist. JNJ-17166864 has low oral bioavailability. JNJ-17166864 can significantly reduce the area of alveolar bone loss in a mouse model of periodontitis induced by Porphyromonas gingivalis infection. JNJ-17166864 can be used in the research of inflammatory diseases such as allergic rhinitis and periodontitis.
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Viscumneoside V
0 ImagesViscumneoside V is a plant-derived anti-inflammatory agent present in Viscum album var. coloratum. Viscumneoside V inhibits the expression of MCP-1 and promotes the production of RANTES in LPS-stimulated immune cells. Viscumneoside V can be used for research related to skin rashes.
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Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA
0 ImagesCat. No.: HY-171685Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated with the linker MC-Vc-PAB-DMEA-PEG2 and the DNA alkylator Duocarmycin SA (HY-12456). Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA can be used in cancer research.
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ECL1i
0 ImagesCat. No.: HY-P11553CAS No.: 1417312-35-6ECL1i is an allosteric, selective CCR2 inhibitor. ECL1i specifically inhibits CCL2-/CCR2-mediated chemotaxis. ECL1i interferes with CCR2-positive cell recruitment and attenuates disease progression in experimental autoimmune encephalomyelitis.
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CCR2-RA
0 ImagesCat. No.: HY-50084CAS No.: 512177-31-0
