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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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 |
| 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]. |
| Synonyms | Hirulog-1, BG-8967 |
| Molecular Weight | 2180.29 |
| Formula | C98H138N24O33 |
| Cas No. | 128270-60-0 |
| Smiles | C([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 | keep 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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