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. CoREST1 promotes tumor formation and tumor stroma interactions in a mouse model of breast cancer.
    Mazumdar, Sohini, Arendt, Lisa M, Phillips, Sarah, Sedic, Maja, Kuperwasser, Charlott, Gill, Grace
    PLoS ONE, 2015;10(3):e0121281.
  2. Secreted Ectodomain of SIGLEC-9 and MCP-1 Synergistically Improve Acute Liver Failure in Rats by Altering Macrophage Polarity
    T Ito, M Ishigami, Y Matsushita, M Hirata, K Matsubara, T Ishikawa, H Hibi, M Ueda, Y Hirooka, H Goto, A Yamamoto
    Sci Rep, 2017;7(0):44043.
  3. Levo-Corydalmine Alleviates Neuropathic Cancer Pain Induced by Tumor Compression via the CCL2/CCR2 Pathway
    Y Hu, ND Kodithuwak, L Zhou, C Li, D Han, W Fang, J Liu, Y Li
    Molecules, 2017;22(6):.
  4. A circadian clock gene, Rev-erbalpha, modulates the inflammatory function of macrophages through the negative regulation of Ccl2 expression.
    Sato S, Sakurai T, Ogasawara J, Takahashi M, Izawa T, Imaizumi K, Taniguchi N, Ohno H, Kizaki T
    J Immunol, 2014;192(1):407-17.
  5. Soluble Siglec-9 suppresses arthritis in a collagen-induced arthritis mouse model and inhibits M1 activation of RAW264.7 macrophages
    Takuya Matsumoto
    Arthritis Res Ther, 2016;18(1):133.
  6. Monocytes infiltrate the pancreas via the MCP-1/CCR2 pathway and differentiate into stellate cells.
    Ino K, Masuya M, Tawara I, Miyata E, Oda K, Nakamori Y, Suzuki K, Ohishi K, Katayama N
    PLoS ONE, 2014;9(1):e84889.
  7. 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.
    Matsubara K, Matsushita Y, Sakai K, Kano F, Kondo M, Noda M, Hashimoto N, Imagama S, Ishiguro N, Suzumura A, Ueda M, Furukawa K, Yamamoto A
    J Neurosci, 2015;35(6):2452-64.
  8. Host gene-encoded severe lung TB: from genes to the potential pathways.
    Ganachari, M, Guio, H, Zhao, N, Flores-Villanueva, P O
    Genes Immun, 2012;13(8):605-20.
  9. Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
    Lourenco S, Teixeira V, Kalber T, Jose R, Floto R, Janes S
    J Immunol, 2015;194(7):3463-74.
  10. Defective TGF-beta signaling in bone marrow-derived cells prevents hedgehog-induced skin tumors.
    Fan Q, Gu D, Liu H, Yang L, Zhang X, Yoder M, Kaplan M, Xie J
    Cancer Res, 2014;74(2):471-83.
  11. The PSMP-CCR2 interactions trigger monocyte/macrophage-dependent colitis
    X Pei, D Zheng, S She, J Ma, C Guo, X Mo, Y Zhang, Q Song, Y Zhang, D Ma, Y Wang
    Sci Rep, 2017;7(1):5107.
  12. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists.
    Mirzadegan et al.
    J.Biol.Chem., 2000;275:25562
  13. CCR2 signaling contributes to ischemia-reperfusion injury in kidney.
    Furuichi et al.
    J.Am.Soc.Nephrol., 2003;14:2503
  14. Blockade of CCR2 ameliorates progressive fibrosis in kidney.
    Kitagawa et al.
    Am.J.Pathol., 2004;165:237
  15. PD-1 blockade inhibits osteoclast formation and murine bone cancer pain
    K Wang, Y Gu, Y Liao, S Bang, CR Donnelly, O Chen, X Tao, AJ Mirando, MJ Hilton, RR Ji
    J. Clin. Invest., 2020;0(0):.

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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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