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BI-2545

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Catalog No. T14560Cas No. 2162961-71-7
Alias BI2545, BI 2545

BI-2545 is a potent and selective autotaxin (ATX) inhibitor with IC50 values of 2.2 nM and 3.4 nM for human and rat ATX, respectively, and reduces plasma LPA levels in rats.

BI-2545

BI-2545

😃Good
Purity: 98.85%
Catalog No. T14560Alias BI2545, BI 2545Cas No. 2162961-71-7
BI-2545 is a potent and selective autotaxin (ATX) inhibitor with IC50 values of 2.2 nM and 3.4 nM for human and rat ATX, respectively, and reduces plasma LPA levels in rats.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$49-In Stock
5 mgPreferential-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.85%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
BI-2545 is a potent and selective autotaxin (ATX) inhibitor with IC50 values of 2.2 nM and 3.4 nM for human and rat ATX, respectively, and reduces plasma LPA levels in rats.
Targets&IC50
ATX (human):2.2 nM, ATX (rat):3.4 nM
In vitro
BI-2545, which exhibits single-digit nanomolar activity in enzyme assays (IC50 = 0.9 nM), demonstrates high potency in rat whole blood (IC50 = 4 nM) and possesses a clean hERG profile along with favorable pharmacokinetic properties [1].
In vivo
In the rat PK/PD model, BI-2545 (10 mg/kg, p.o.) demonstrated a significant reduction in LPA levels, decreasing total plasma LPA by up to 90% [1].
SynonymsBI2545, BI 2545
Chemical Properties
Molecular Weight527.42
FormulaC23H19F6N5O3
Cas No.2162961-71-7
SmilesC(NC(=O)C=1C=C2C(=CC1)N=NN2)[C@@H]3[C@@]4([C@]3(CN(C(OCC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O)C4)[H])[H]
Relative Density.1.513 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 200 mg/mL (379.2 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8960 mL9.4801 mL18.9602 mL94.8011 mL
5 mM0.3792 mL1.8960 mL3.7920 mL18.9602 mL
10 mM0.1896 mL0.9480 mL1.8960 mL9.4801 mL
20 mM0.0948 mL0.4740 mL0.9480 mL4.7401 mL
50 mM0.0379 mL0.1896 mL0.3792 mL1.8960 mL
100 mM0.0190 mL0.0948 mL0.1896 mL0.9480 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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