Catalog Number: 2089
Chemical Name: 1'-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one hydrochloride
Biological Activity
CCR2-selective chemokine receptor antagonist (IC50 values are 0.36 and 17.8 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC50 values of 32 nM and 1.7 μM respectively. Also inhibits α1A, α1D and 5-HT1A receptors.
Technical Data
  • M.Wt:
    426.86
  • Formula:
    C21H21F3N2O2.HCl
  • Solubility:
    Soluble to 75 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    1173022-16-6
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. Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'piperidin]-2(1H)-ones.
    Clark et al.
    J.Med.Chem., 1983;26:657
  2. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists.
    Mirzadegan et al.
    J.Biol.Chem., 2000;275:25562
Citations:

The citations listed below are publications that use Tocris products. Selected citations for RS 102895 hydrochloride include:

2 Citations: Showing 1 - 2
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  1. Tumor-derived CXCL8 signaling augments stroma-derived CCL2-promoted proliferation and CXCL12-mediated invasion of PTEN-deficient prostate cancer cells.
    Authors: Maxwell Et al.
    Oncotarget 2014;5:4895
  2. CCR2(+) monocytes infiltrate atrophic lesions in age-related macular disease and mediate photoreceptor degeneration in experimental subretinal inflammation in Cx3cr1 deficient mice.
    Authors: Sennlaub Et al.
    EMBO Mol Med 2013;5:1775

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