1. Metabolic Enzyme/Protease Immunology/Inflammation Anti-infection
  2. Thrombin Interleukin Related RSV
  3. Bivalirudin TFA

Bivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others.

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

Custom Peptide Synthesis

Bivalirudin TFA Chemical Structure

Bivalirudin TFA Chemical Structure

CAS No. : 1191386-55-6

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Bivalirudin TFA:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others[1][2][3][4].

IC50 & Target[2]

IL-6

 

IL-5

 

In Vitro

Bivalirudin (30 μg/mL; 10 min) TFA inhibits Thrombin (HY-114164)-induced S1PR2 upregulation and endothelial hyperpermeability, and reverses the abnormal distribution of cytoskeletal proteins and β-catenin in HUVECs[1].

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

Western Blot Analysis[1]

Cell Line: HUVECs treated Thrombin (HY-114164)
Concentration: 30 μg/mL
Incubation Time: 10 min
Result: Inhibited the level of S1PR2.
In Vivo

Bivalirudin (2 mg/kg; intravenous injection; every other day; 2 weeks) TFA exhibits antiviral activity against respiratory syncytial virus in neonatal C57BL/6 mice[2].
Bivalirudin (2 mg/kg; intravenous injection; single dose) TFA inhibits thrombosis in mice[3].

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

Animal Model: C57BL/6 mice aged 5-7 days old treated respiratory syncytial virus (RSV)[2]
Dosage: 2 mg/kg
Administration: Intravenous injection; every other day; 2 weeks
Result: Significantly reduced cellular infiltration, inflammatory cytokines (e.g., IL-5, IL-6, CXCL1), and abnormal clotting parameters (e.g., D-dimer, soluble thrombomodulin) in RSV-infected lungs.
Normalized viral copy numbers and reversed histopathological changes such as nuclear pyknosis in pneumocytes.
Animal Model: P2Y12-- and WT mice with thrombosis induced by perfusion through type III collagen- or tissue factor-coated capillary chambers, and P2Y12+- mice with mesenteric artery injury induced by 12.5% FeCl3 solution[3]
Dosage: 2 mg/kg
Administration: Intravenous injection; single dose
Result: Significantly inhibited thrombus volume in P2Y12-- mice in the type III collagen-induced thrombosis model but had no significant effect in wild-type mice.
Inhibited thrombosis in both WT and P2Y12-- mice in the tissue factor-induced thrombosis model.
Delayed the time of thrombus appearance and vessel occlusion, but could not completely prevent vessel occlusion in wild-type mice in the FeCl3-induced mesenteric artery injury model in P2Y12+- mice.
Clinical Trial
Molecular Weight

2294.34

Formula

C98H138N24O33.C2HF3O2

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{d-Phe}-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu

Sequence Shortening

{d-Phe}-PRPGGGGNGDFEEIPEEYL

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (21.79 mM)

DMSO : ≥ 31 mg/mL (13.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4359 mL 2.1793 mL 4.3586 mL
5 mM 0.0872 mL 0.4359 mL 0.8717 mL
View the Complete Stock Solution Preparation Table

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (1.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (1.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (21.79 mM); Clear solution; Need ultrasonic

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

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.89%

References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.4359 mL 2.1793 mL 4.3586 mL 10.8964 mL
5 mM 0.0872 mL 0.4359 mL 0.8717 mL 2.1793 mL
10 mM 0.0436 mL 0.2179 mL 0.4359 mL 1.0896 mL
H2O 15 mM 0.0291 mL 0.1453 mL 0.2906 mL 0.7264 mL
20 mM 0.0218 mL 0.1090 mL 0.2179 mL 0.5448 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Bivalirudin TFA
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