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Bivalirudin

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Catalog No. T5519Cas No. 128270-60-0
Alias Hirulog-1, BG-8967

Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.

Bivalirudin

Bivalirudin

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Purity: 99.97%
Catalog No. T5519Alias Hirulog-1, BG-8967Cas No. 128270-60-0
Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$29-In Stock
10 mg$40-In Stock
25 mg$90-In Stock
50 mg$160-In Stock
100 mg$280-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.97%
Color:White
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Product Introduction

Bioactivity
Description
Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.
Targets&IC50
α-thrombin:2.56 nM (Ki, cell free)
In vitro
Whereas 0.1 microM-hirudin and 0.1 microM-Bivalirudin (i.e. less than 10% of the concentration of prothrombin in plasma) inhibited Factor X, Factor V, and prothrombin activation. Concentrations of hirudin and hirulog-1 equimolar to and 5 times greater than those of alpha-thrombin respectively abrogated Factor V activation by exogenous alpha-thrombin [2].
In vivo
Deposition in aspirin-treated groups receiving low-, medium-, and high-dose Bivalirudin decreased in a dose-dependent manner by 37%, 44%, and 56%, respectively. As the dose of Bivalirudin was increased, the plasma Bivalirudin levels and activated partial thromboplastin time ratios (final: initial) also increased in a dose-dependent manner. The mean plasma Bivalirudin levels ranged from 0.74 micrograms/ml in the low-dose Bivalirudin group to 2.55 micrograms/ml in the high-dose Bivalirudin group, and the corresponding activated partial thromboplastin time ratios were 1.5 and 3.3 [3].
Animal Research
Animals were randomly assigned to one of five groups: control (no aspirin or hirulog); aspirin alone (10 mg/kg); aspirin plus low-dose hirulog (0.2 mg/kg bolus followed by 0.5 mg/kg/hr); aspirin plus medium-dose hirulog (0.4 mg/kg bolus followed by 1.0 mg/kg/hr); or aspirin plus high-dose hirulog (0.6 mg/kg bolus followed by 1.5 mg/kg/hr). Hirulog was infused before surgery and continued until termination of the experiment 30 minutes after endarterectomy [3].
SynonymsHirulog-1, BG-8967
Chemical Properties
Molecular Weight2180.29
FormulaC98H138N24O33
Cas No.128270-60-0
SmilesC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CC1=CC=CC=C1)NC([C@@H](NC(CNC([C@@H](NC(CNC(CNC(CNC(CNC(=O)[C@H]2N(C([C@@H](NC(=O)[C@H]3N(C([C@@H](CC4=CC=CC=C4)N)=O)CCC3)CCCNC(=N)N)=O)CCC2)=O)=O)=O)=O)CC(N)=O)=O)=O)CC(O)=O)=O)=O)CCC(O)=O)=O)CCC(O)=O)=O)[C@H](CC)C)(=O)N5[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC6=CC=C(O)C=C6)C(N[C@@H](CC(C)C)C(O)=O)=O)=O)CCC(O)=O)=O)CCC(O)=O)=O)CCC5
Relative Density.1.52 g/cm3
Sequence{d-Phe}-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-ILE-Pro-Glu-Glu-Tyr-Leu
Sequence Short{d-Phe}-PRPGGGGNGDFEEIPEEYL
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 10 mM, Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.4587 mL2.2933 mL4.5865 mL22.9327 mL
5 mM0.0917 mL0.4587 mL0.9173 mL4.5865 mL
10 mM0.0459 mL0.2293 mL0.4587 mL2.2933 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:
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2 Enter the in vivo formulation:
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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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