Sibrafiban
Based on 1 Customer Validation
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
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- Pureza: 99.67%
- No. CAS: 172927-65-0
- Fòrmula: C20H28N4O6
- Peso molecular:420.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
Glycoprotein IIb/IIIa receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
>50 μM
Compound: sibrafiban
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Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to fibronectin
Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to fibronectin
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[PMID: 15056002] |
| HUVEC | IC50 |
>50 μM
Compound: sibrafiban
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Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to vitronectin
Inhibition of Human umbilical vein endothelial cells (HUVEC) adhesion to vitronectin
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[PMID: 15056002] |
The effects of site occupancy by Sibrafiban on platelet activation are assessed using P-selectin expression, fibrinogen binding and microaggregate formation. Sibrafiban inhibits ADP and TRAP-stimulated fibrinogen binding and microaggregate formation in a concentration-dependent manner, whereas P-selectin expression is relatively unaltered. A decrease in site occupancy from peak to trough of Sibrafiban does not result in increased activation of platelets[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 172927-65-0
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Appearance Solid
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Peso molecular 420.47
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Fòrmula C20H28N4O6
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Color White to off-white
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SMILES
O=C(OCC)COC1CCN(C([C@@H](NC(C2=CC=C(/C(N)=N/O)C=C2)=O)C)=O)CC1.[(Z)]
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Synonyms
RO 48-3657
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (118.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. M Dooley, et al. Sibrafiban. Drugs. 1999 Feb;57(2):225-30; discussion 231-2. [Content Brief]
[2]. B Wittke, et al. Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin. Br J Clin Pharmacol. 2000 Mar;49(3):231-9. [Content Brief]
[3]. Jeffrey T Billheimer, et al. Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy. Thromb Res. 2002 Sep 15;107(6):303-17. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3783 mL | 11.8915 mL | 23.7829 mL | 59.4573 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL | 11.8915 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 mL | 5.9457 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5855 mL | 3.9638 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | 2.9729 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9819 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4864 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1891 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |
Sibrafiban Related Classifications
HY-10309 Related Classifications
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