BX471

Catalog No.S7604 Batch:S760402

Technical Data

Formula

C₂₁H₂₄ClFN₄O₃

Molecular Weight

434.89

CAS No.

217645-70-0

Solubility (25°C)*

In vitro

DMSO

87 mg/mL (200.05 mM)

Ethanol

22 mg/mL (50.58 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.725mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 14.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.35mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 87 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.<a class="sref" href="#s_ref">[1]</a><a class="sref" href="#s_ref">[2]</a>

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

Protocol (from reference)

Cell Assay:^{<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 Study:^{^[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.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

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 Study:^{^[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.

References

Selleck's BX471 has been cited by 1 publication

SATB1 prevents immune cell infiltration by regulating chromatin organization and gene expression of a chemokine gene cluster in T cells [ Commun Biol, 2024, 7(1):1304]	PubMed: 39394451

SATB1 prevents immune cell infiltration by regulating chromatin organization and gene expression of a chemokine gene cluster in T cells [ Commun Biol, 2024, 7(1):1304]

PubMed: 39394451

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.