Catalog Number: 2517
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 Activity
Extremely 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.
Technical Data
  • M.Wt:
    417.5
  • Formula:
    C25H27N3O3
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    300816-15-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists.
    Mirzadegan et al.
    J.Biol.Chem., 2000;275:25562
  2. CCR2 signaling contributes to ischemia-reperfusion injury in kidney.
    Furuichi et al.
    J.Am.Soc.Nephrol., 2003;14:2503
  3. Blockade of CCR2 ameliorates progressive fibrosis in kidney.
    Kitagawa et al.
    Am.J.Pathol., 2004;165:237
Citations:

The citations listed below are publications that use Tocris products. Selected citations for RS 504393 include:

12 Citations: Showing 1 - 10
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  1. 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
  2. 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
  3. 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
  4. CoREST1 Promotes Tumor Formation and Tumor Stroma Interactions in a Mouse Model of Breast Cancer.
    Authors: Mazumdar Et al.
    PLoS One 2015;10:e0121281
  5. 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
  6. IL-33-induced hematopoietic stem and progenitor cell mobilization depends upon CCR2.
    Authors: Kim Et al.
    J Immunol 2014;193:3792
  7. Obesity promotes breast cancer by CCL2-mediated macrophage recruitment and angiogenesis.
    Authors: Arendt Et al.
    J Biol Chem 2013;73:6080
  8. 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
  9. 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
  10. CCR2 chemokine receptor signaling mediates pain in experimental osteoarthritis.
    Authors: Miller Et al.
    Proc Natl Acad Sci U S A 2012;109:20602
  11. 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
  12. 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.
    Diabetologia 2009;52:972
Expand to show all 12 Citations

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