Chemical Name: 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
Biological ActivityExtremely selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists.
Mirzadegan et al.
CCR2 signaling contributes to ischemia-reperfusion injury in kidney.
Furuichi et al.
Blockade of CCR2 ameliorates progressive fibrosis in kidney.
Kitagawa et al.
Citations for RS 504393
The citations listed below are publications that use Tocris products. Selected citations for RS 504393 include:
15 Citations: Showing 1 - 10
Macrophages orchestrate breast cancer early dissemination and metastasis.
Nat Commun 2018;9(1):21
Concomitant type I IFN and M-CSF signaling reprograms monocyte differentiation and drives pro-tumoral arginase production.
Authors: Tong Et al.
The RS504393 Influences the Level of Nociceptive Factors and Enhances Opioid Analgesic Potency in Neuropathic Rats.
Authors: Kwiatkowski Et al.
J Neuroimmune Pharmacol 2017;
Inhibiting the mobilization of Ly6C(high) monocytes after acute myocardial infarction enhances the efficiency of mesenchymal stromal cell transplantation and curbs myocardial remodeling.
Authors: Lu Et al.
J Neurosci 2015;7:587
Secreted ectodomain of sialic acid-binding Ig-like lectin-9 and monocyte chemoattractant protein-1 promote recovery after rat spinal cord injury by altering macrophage polarity.
Authors: Matsubara Et al.
Cancer Res 2015;35:2452
Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
Authors: Lourenco Et al.
J Immunol 2015;194:3463
CoREST1 Promotes Tumor Formation and Tumor Stroma Interactions in a Mouse Model of Breast Cancer.
Authors: Mazumdar Et al.
PLoS One 2015;10:e0121281
Functional Interaction between Angiotensin II Receptor Type 1 and Chemokine (C-C Motif) Receptor 2 with Implications for Chronic Kidney Disease.
Authors: Ayoub Et al.
PLoS One 2015;10:e0119803
IL-33-induced hematopoietic stem and progenitor cell mobilization depends upon CCR2.
Authors: Kim Et al.
J Immunol 2014;193:3792
Obesity promotes breast cancer by CCL2-mediated macrophage recruitment and angiogenesis.
Authors: Arendt Et al.
J Biol Chem 2013;73:6080
Expression and function of CCL2/CCR2 in rat micturition reflexes and somatic sensitivity with urinary bladder inflammation.
Authors: Arms Et al.
Am J Physiol Renal Physiol 2013;305:F111
Chemokine CCL2 and its receptor CCR2 in the medullary dorsal horn are involved in trigeminal neuropathic pain.
Authors: Zhang Et al.
J Neuroinflammation 2012;9:136
CCR2 chemokine receptor signaling mediates pain in experimental osteoarthritis.
Authors: Miller Et al.
Proc Natl Acad Sci U S A 2012;109:20602
Endothelin-1 increases collagen accumulation in renal mesangial cells by stimulating a chemokine and cytokine autocrine signaling loop.
Authors: Simonson and Ismail-Beigi
Br J Pharmacol 2011;286:11003
Inhibition of the chemokine (C-C motif) ligand 2/chemokine (C-C motif) receptor 2 pathway attenuates hyperglycaemia and inflammation in a mouse model of hepatic steatosis and lipoatrophy.
Authors: Yang Et al.
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Receptor antagonists (SB225002: for CXCR2, AMD3465: for CXCR4, RS504393: for CCR2 and Maraviroc: for CCR5) at 10 μM