BX471

Catalog No.S7604 Synonyms: ZK811752, BAY 865047, SH T 04268H

For research use only.

BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.

BX471 Chemical Structure

CAS No. 217645-70-0

Purity & Quality Control

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Biological Activity

Description

BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.

Targets
CCR1 [1]
(in MIP-1α binding assay)
CCR1 [1]
(in MCP-3 binding assay)
1 nM(ki) 5.5 nM(ki)
In vitro

By displacing the ligand binding to CC chemokine receptor-1 (CCR1), BX 471, a potent antagonist, can inhibit the effects medicated by CCR1. In addition, BX-471 exhibits anti-allergic effect by increasing Treg cell population.<sup><a class="sref" href="#s_ref">[1]</a></sup><sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

For fasted dogs, the half-life for BX 471 was approximately 3 h, with an oral bioavailability of approximately 60%. In rats of EAE model, CCR1 antagonist, BX 471, dose-dependently decreased the severity of the disease.<sup><a class="sref" href="#s_ref">[1]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Cell lines: THP-1- or CCR1-transfected HEK293 cells
  • Concentrations: 10 µM
  • Incubation Time: 24 h
  • Method:

    Binding assays were performed by filtration. Radiolabeled chemokines at a final concentration of approximately 0.1–0.2 nM were used as ligand. HEK293 cells expressing human CCR1 at 8,000 or 300,000 cells per assay point were used as the receptor source. Nonspecific binding was determined in the presence of 100 nM unlabeled chemokine. The binding data were curve-fitted with the computer program IGOR (Wavemetrics) to determine the affinity and number of sites. To demonstrate that CCR1 antagonism by BX 471 was not due to the cellular toxicity of the compound, THP-1- or CCR1-transfected HEK293 cells were treated with BX 471 at concentrations up to 10 µM for 24 h, and cellular toxicity was monitored by measuring WST-1 staining. No significant toxicity was observed.

Animal Research:

[1]

  • Animal Models: Fasted male beagle dogs; Male Lewis Rats of EAE model
  • Dosages: 4 mg/kg (for fasted male beagle dogs); 20 and 50 mg/kg (for Male Lewis Rats)
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 434.89
Formula

C21H24ClFN4O3

CAS No. 217645-70-0
Storage 3 years -20°C powder
2 years -80°C in solvent

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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