製品の概要

  • 製品名

    RS 504393, CCR2 chemokine receptor antagonist
  • 製品の詳細

    Highly selective CCR2 chemokine receptor antagonist
  • 生理活性の詳細

    Highly selective CCR2 chemokine receptor antagonist (IC50 = 89 nM). Shows 700-fold greater binding for CCR2 vs. CCR1. Inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
  • 精製度

    > 98%
  • CAS 番号

    300816-15-3
  • 構造式

    Chemical Structure

製品の特性

参考文献

This product has been referenced in:

  • Kitagawa K  et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. Am J Pathol 165:237-46 (2004). Read more (PubMed: 15215179) »
  • Furuichi K  et al. CCR2 signaling contributes to ischemia-reperfusion injury in kidney. J Am Soc Nephrol 14:2503-15 (2003). Read more (PubMed: 14514728) »
  • Mirzadegan T  et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem 275:25562-71 (2000). Read more (PubMed: 10770925) »

レビューと Q&A

Question
Answer

The amount of product required depends on many factors including target accessibility, cell permeability, duration of incubation, and type of cells or assay used, it is best to survey the literature to determine the IC50, EC50 or Ki. For an inhibitor, if published Ki or, IC50 values are known, we recommend that you use 5 to 10 times higher than these values to maximally inhibit enzyme or receptor activity. If there are no published values we recommend that you perform dose-response experiments (running appropriate controls) and use Michaelis-Menten kinetics to determine the Ki value.

From my quick research, I found that for the pharmacological inhibition of CCR2, the specific CCR2 antagonist RS 504393 has a IC50 for CCR2 of 98 nM. RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 of 330 nM.

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