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250mg | ||
500mg |
ln Vitro |
Fradafiban is a non-peptide mimic of the arginine-glycine-aspartate recognition sequence. Fradafiban binds to the human platelet GP IIb/IIIa complex with great affinity and selectivity and efficiently suppresses human platelet aggregation in vitro. Fradafiban reversibly binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM [1].
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ln Vivo |
Fradafiban exhibits relatively little oral action, which may be related to its greater polarity and thus low absorption when taken orally [1].
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References |
[1]. Müller TH, et al. Profound and sustained inhibition of platelet aggregation by Fradafiban, a nonpeptide platelet glycoprotein IIb/IIIa antagonist, and its orally active prodrug, Lefradafiban, in men. Circulation. 1997 Aug 19;96(4):1130-8.
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Molecular Formula |
C20H21N3O4
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Molecular Weight |
367.39800
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CAS # |
148396-36-5
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Related CAS # |
Fradafiban hydrochloride
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(O)C[C@H]1C(N[C@H](COC2=CC=C(C3=CC=C(C(N)=N)C=C3)C=C2)C1)=O
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~180 mg/mL (~489.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (6.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (6.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (6.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | |
5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | |
10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.