RS 504393

Catalog # Availability Size / Price Qty
2517/10
RS 504393 | CAS No. 300816-15-3 | Chemokine Receptor Antagonists
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Description: Highly selective CCR2 chemokine receptor antagonist

Chemical Name: 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one

Purity: ≥99%

Product Details
Citations (15)
Supplemental Products
Reviews

Biological Activity

RS 504393 is an 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

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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

  1. Macrophages orchestrate breast cancer early dissemination and metastasis.
    Authors: Linde
    Nat Commun  2018;9(1):21
  2. Concomitant type I IFN and M-CSF signaling reprograms monocyte differentiation and drives pro-tumoral arginase production.
    Authors: Tong Et al.
    EBioMedicine  2018;
  3. The RS504393 Influences the Level of Nociceptive Factors and Enhances Opioid Analgesic Potency in Neuropathic Rats.
    Authors: Kwiatkowski Et al.
    J Neuroimmune Pharmacol  2017;
  4. 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
  5. 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
  6. 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
  7. CoREST1 Promotes Tumor Formation and Tumor Stroma Interactions in a Mouse Model of Breast Cancer.
    Authors: Mazumdar Et al.
    PLoS One  2015;10:e0121281
  8. 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
  9. IL-33-induced hematopoietic stem and progenitor cell mobilization depends upon CCR2.
    Authors: Kim Et al.
    J Immunol  2014;193:3792
  10. Obesity promotes breast cancer by CCL2-mediated macrophage recruitment and angiogenesis.
    Authors: Arendt Et al.
    J Biol Chem  2013;73:6080

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