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BX471 (ZK-811752) CCR1 Antagonist

Name: BX471 (ZK-811752)
Brand: Selleck Chemicals
SKU: S7604
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S7604

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.

Chemical Structure

Molecular Weight: 434.89

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other CCR Inhibitors	Cenicriviroc ZK756326 2HCl INCB3344 Vicriviroc Malate SB-297006 R243 Adaptavir (DAPTA) RS102895 BMS-813160 AZD2098

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (200.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (10.00mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.725mg/ml (1.67mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	434.89	Formula	C₂₁H₂₄ClFN₄O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	217645-70-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ZK811752, BAY 865047, SH T 04268H			Smiles	CC1CN(CCN1C(=O)COC2=C(NC(N)=O)C=C(Cl)C=C2)CC3=CC=C(F)C=C3

Mechanism of Action

Targets/IC₅₀/Ki	CCR1 (in MIP-1α binding assay) 1 nM(ki) CCR1 (in MCP-3 binding assay) 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>
References	[1] https://pubmed.ncbi.nlm.nih.gov/10748002/ [2] https://pubmed.ncbi.nlm.nih.gov/32801828/

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