2. Metabolic Enzyme/Protease
  3. Thrombin
  4. Dabigatran

Dabigatran  (Synonyms: BIBR 953; BIBR 953ZW)

Cat. No.: HY-10163 Purity: 98.06%
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Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).

For research use only. We do not sell to patients.

CAS No. : 211914-51-1

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Dabigatran:

Dabigatran Related Antibodies

Top Publications Citing Use of Products

    Dabigatran purchased from MedChemExpress. Usage Cited in: Elife. 2022 Mar 23:11:e77444.  [Abstract]

    Vero cells with rVSVG/SARS-CoV-2 pseudovirus pretreated for 4 hr with 10 µM Camostat, Nafamostat, Dabigatran, or Otamixaban, compared with uninfected or infected/untreated cells.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].

    IC50 & Target

    Ki: 4.5 nM (thrombin)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    25.3 μM
    Compound: Dabigatran
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    		[PMID: 23241029]
    HEK293 IC50
    4.7 μM
    Compound: Dabigatran
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    		[PMID: 23241029]
    HEK293 IC50
    8.1 μM
    Compound: Dabigatran
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    		[PMID: 23241029]
    Platelet EC50
    0.007 μM
    Compound: Dabigatran
    Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
    Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
    		[PMID: 36462436]
    Platelet EC50
    0.029 μM
    Compound: Dabigatran
    Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
    Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
    		[PMID: 36462436]
    Platelet IC50
    0.6 μM
    Compound: Dabigatran
    Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation
    Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation
    		[PMID: 34902735]
    In Vitro

    Dabigatran (BIBR 953) shows concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human platelet-poor plasma at concentrations of 0.23, 0.83 and 0.18 μM, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dabigatran Related Antibodies
    In Vivo

    Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED50 of 0.033 mg/kg in Wessler model[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male rats (Wessler model)[3]
    Dosage: 0.01, 0.03, 0.05 and 0.1 mg/kg
    Administration: Intravenous injection
    Result: Inhibited clot formation with an ED50 of 0.033 mg/kg.
    Clinical Trial
    Molecular Weight

    471.51

    Formula

    C25H25N7O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    N=C(N)C(C=C1)=CC=C1NCC2=NC3=CC(C(N(CCC(O)=O)C4=NC=CC=C4)=O)=CC=C3N2C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    0.1 M HCl : 12.5 mg/mL (26.51 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

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

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1208 mL 10.6042 mL 21.2085 mL
    5 mM 0.4242 mL 2.1208 mL 4.2417 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    0.1 M HCl 1 mM 2.1208 mL 10.6042 mL 21.2085 mL 53.0211 mL
    5 mM 0.4242 mL 2.1208 mL 4.2417 mL 10.6042 mL
    10 mM 0.2121 mL 1.0604 mL 2.1208 mL 5.3021 mL
    15 mM 0.1414 mL 0.7069 mL 1.4139 mL 3.5347 mL
    20 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6511 mL
    25 mM 0.0848 mL 0.4242 mL 0.8483 mL 2.1208 mL
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    Dabigatran Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dabigatran211914-51-1BIBR 953 BIBR 953ZWBIBR953BIBR-953ThrombinInhibitorinhibitorinhibit

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