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BI-2545

Name: BI-2545
Brand: TargetMol
SKU: T14560
Rating: 4.5 (1 reviews)

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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

🥰Excellent

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.

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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 (rat):3.4 nM, ATX (human):2.2 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].
Synonyms	BI2545, BI 2545

Chemical Properties

Molecular Weight	527.42
Formula	C₂₃H₁₉F₆N₅O₃
Cas No.	2162961-71-7
Smiles	C(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)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

store 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

	1mg	5mg	10mg	50mg
1 mM	1.8960 mL	9.4801 mL	18.9602 mL	94.8011 mL
5 mM	0.3792 mL	1.8960 mL	3.7920 mL	18.9602 mL
10 mM	0.1896 mL	0.9480 mL	1.8960 mL	9.4801 mL
20 mM	0.0948 mL	0.4740 mL	0.9480 mL	4.7401 mL
50 mM	0.0379 mL	0.1896 mL	0.3792 mL	1.8960 mL
100 mM	0.0190 mL	0.0948 mL	0.1896 mL	0.9480 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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