Bivalirudin Trifluoroacetate |
| Catalog No.GC10448 |
A thrombin inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 128270-60-0
Sample solution is provided at 25 µL, 10mM.
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BivalirudinTrifluoroacetate is a specific, reversible and direct thrombin inhibitor with a predictable anticoagulant effect.
In patients with normal or mildly impaired renal function, bivalirudin exihibited several notable mechanistic advantages when compared with unfractionated heparin. Bivalirudin showed activity against clot-bound thrombin, inhibition of thrombin-induced platelet activation, short plasma half-life (25 minutes)[1]. Bivalirudin inhibited both circulating thrombin and fibrin bound thrombin directly by binding to thrombin catalytic site and anion-binding exosite I in a concentration-dependent manner. Bivalirudin prolonged activated partial thromboplastin time, prothrombin time, thrombin time and activated clotting time (ACT). ACT levels activated by bivalirudin showed no correlation with its clinical efficacy [1]. When compared to heparin alone or heparin in combination with-a GpIIb/IIIa inhibitor, bivalirudin had shown less in-hospital major bleeding. Bivalirudin was safe and effective during percutaneous coronary intervention (PCI) in patients with heparin-induced thrombocytopenia, indicated the safety and efficacy of bivalirudin [1].
Reference:
[1]. Shammas N W. Bivalirudin: pharmacology and clinical applications[J]. Cardiovascular drug reviews, 2005, 23(4): 345-360.
| In vitro experiment [1]: | |
|
Samples |
Platelet-poor plasma |
|
Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
1.5 ~ 30 μg/mL |
|
Applications |
In platelet-poor plasma, Bivalirudin dose-dependently delayed thrombin formation regardless of the activators. Under actin activation, thrombin peak levels decreased progressively (21.5% ± 9.2% at 1.5 μg/mL to 69.9% ± 12.3% at 30 μg/mL). With tissue factor as a trigger, the decrease was more gradual. The peak level of thrombin was only reduced by 29.4% ± 6.2% at 30 μg/mL. |
| Animal experiment [2]: | |
|
Animal models |
A thromboplastin-induced thrombosis mouse model |
|
Dosage form |
1 μmol/kg; i.v. |
|
Applications |
In a thromboplastin-induced lung thrombosis mouse model, Bivalirudin micelles were accumulated in lung thrombi 10-fold more than free Bivalirudin. Moreover, Bivalirudin micelles significantly prolonged the half-life time, increasing the bioavailability of Bivalirudin. In addition, Bivalirudin micelles showed significantly higher anticoagulant activity than free Bivalirudin in both the lung thrombosis model and the ferric chloride-induced carotid artery thrombosis model. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Tanaka KA, Szlam F, Sun HY, Taketomi T, Levy JH. Thrombin generation assay and viscoelastic coagulation monitors demonstrate differences in the mode of thrombin inhibition between unfractionated heparin and bivalirudin. Anesth Analg. 2007 Oct;105(4):933-9. [2]. She ZG, Liu X, Kotamraju VR, Ruoslahti E. Clot-targeted micellar formulation improves anticoagulation efficacy of bivalirudin. ACS Nano. 2014 Oct 28;8(10):10139-49. | |
| Cas No. | 128270-60-0 | SDF | |
| Chemical Name | (1Z,4Z,7Z,10Z,13Z,15S,16Z,19Z,21S,22Z,24S,25Z,27S,28Z,30S)-1-((S)-1-((S)-2-((Z)-(((S)-1-((R)-2-amino-3-phenylpropanoyl)pyrrolidin-2-yl)(hydroxy)methylene)amino)-5-guanidinopentanoyl)pyrrolidin-2-yl)-24-benzyl-30-((Z)-(((2S,3S)-1-((S)-2-((1Z,3S,4Z,6S,7Z,9S | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/C/N=C(O)/C/N=C(O)/C/N=C(O)/C/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@]2([H])CCCN2C([C@@](N)([H])CC3=CC=CC=C3)=O)([H])CCCNC(N)=N)=O)([H])CC(O)=N)([H])CC(O)=O)([H | ||
| Formula | C98H138N24O33 | M.Wt | 2180.29 |
| Solubility | ≥ 54.5 mg/mL in DMSO with gentle warming, ≥ 42 mg/mL in EtOH with gentle warming, ≥ 86.2 mg/mL in Water with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.4587 mL | 2.2933 mL | 4.5865 mL |
| 5 mM | 0.0917 mL | 0.4587 mL | 0.9173 mL |
| 10 mM | 0.0459 mL | 0.2293 mL | 0.4587 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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