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Dabigatran etexilate

Name: Dabigatran etexilate
Brand: TargetMol
SKU: T0389
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0389Cas No. 211915-06-9

Alias BIBR 1048

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

Dabigatran etexilate

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Purity: 99.98%

Catalog No. T0389Alias BIBR 1048Cas No. 211915-06-9

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$48	In Stock	In Stock
10 mg	$68	In Stock	In Stock
50 mg	$89	In Stock	In Stock
100 mg	$120	In Stock	In Stock
200 mg	$175	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$73	In Stock	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:99.98%

Color:White

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COA LCMS HNMR

Product Introduction

Dabigatran etexilate AI Summary

Dabigatran etexilate exhibits a wide range of bioactivities including antithrombotic, antiviral, and enzyme inhibitory effects. Pharmacokinetic studies in humans show a volume of distribution (Vd) of 0.85 L∙kg⁻¹ and a volume of distribution at steady state (Vdss) of 68.6 L∙kg⁻¹ when administered intravenously at a bolus dose of 5.5 mg. The compound has relatively low oral bioavailability in humans (6.0-7.2%) and in rats (7.2%). It demonstrates antiplatelet activity by inhibiting thrombin-induced platelet aggregation with IC50 values ranging from 326 nM in humans to 337 nM in rabbit models. Additionally, it shows antithrombotic effects in various rat models with ED50 values ranging from 4.4 mg∙kg⁻¹ to 7.8 µmol∙kg⁻¹. Dabigatran etexilate also has moderate aqueous solubility at different pH levels and a log D value of 3.7 at pH 7, indicating moderate distribution. It has been shown to effectively inhibit human thrombin with IC50 values as low as 2.63 nM and 2.61 nM in chromogenic assays. Apart from its anticoagulant properties, Dabigatran etexilate demonstrates antiviral activities against both Ebola virus and SARS-CoV-2. For SARS-CoV-2, it showed a hit score of 0.242 in HRCE cells and variable inhibition of virus-induced cytotoxicity in VERO-6 cells with IC50 values exceeding 20000 nM. Moreover, it exhibits moderate clearance (CL) of 155.0 ml/min and has been tested for various enzyme inhibitions, including human HDAC6 with a 26.29% inhibition rate. Its broad binding affinities include human thrombin and other receptors like SLC6A2, ADORA3, SCN5A, and NR1I2. Collectively, these characteristics highlight Dabigatran etexilate's potential as an antithrombotic, antiviral, and enzyme inhibitory agent..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.
Targets&IC50	DTI:4.5 nM (Ki)
In vitro	Dabigatran has a concentration-dependent anticoagulant effect in various animals.Dabigatran reversibly inhibits human thrombin (Ki: 4.5 nM) and thrombin-induced platelet aggregation (IC50= 10 nM).
In vivo	Dabigatran has a concentration-dependent anticoagulant effect in various animals.Dabigatran reversibly inhibits human thrombin (Ki: 4.5 nM) and thrombin-induced platelet aggregation (IC50= 10 nM).
Synonyms	BIBR 1048

Chemical Properties

Molecular Weight	627.73
Formula	C₃₄H₄₁N₇O₅
Cas No.	211915-06-9
Smiles	CCCCCCOC(=O)N\N=C\c1ccc(NCc2nc3cc(ccc3n2C)C(=O)N(CCC(=O)OCC)c2ccccn2)cc1
Relative Density.	1.24 g/cm3

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: 250 mg/mL (398.26 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 10 mg/mL (15.93 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.37 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5930 mL	7.9652 mL	15.9304 mL	79.6521 mL
5 mM	0.3186 mL	1.5930 mL	3.1861 mL	15.9304 mL
10 mM	0.1593 mL	0.7965 mL	1.5930 mL	7.9652 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.0797 mL	0.3983 mL	0.7965 mL	3.9826 mL
50 mM	0.0319 mL	0.1593 mL	0.3186 mL	1.5930 mL
100 mM	0.0159 mL	0.0797 mL	0.1593 mL	0.7965 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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