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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Prasugrel (formerly CS-747, PCR-4099; LY-640315; trade name Effient; Prasita), a piperazine derivative, is an irreversible and thienopyridine-based ADP receptor (P2Y12) antagonist approved as an antiplatelet and anticoagulant drug used for the reduction of thrombotic cardiovascular events. As a platelet aggregation inhibitor, it is used to prevent thrombosis in patients with acute coronary syndrome; unstable angina and myocardial infarction, as well as in those undergoing percutaneous coronary interventions. Prasugrel was also approved for use in Europe in February 2009 and On July 10, 2009 in the US for for the reduction of thrombotic cardiovascular events in patients with acute coronary syndrome who are to be managed with PCI.
ln Vitro |
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ln Vivo |
With an IC50 value of 1.8 μM, the active metabolite of prasugrel inhibits the platelet aggregation generated by adenosine ADP (10 μM) in vitro in rat platelets [2]. In comparison to clopidogrel, prasugrel operates more quickly and effectively in the body. The body must undergo metabolic processing on the inactive prodrug prasugrel in order to create the active antiplatelet metabolite. The intestines absorb prasugrel very quickly. The active metabolite's plasma concentration increases to a maximum in 1 hour, becomes effective in 1-2 hours, and maximally inhibits platelet aggregation following oral administration of a conventional loading dose of 60 mg [1].
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Animal Protocol |
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References |
[1]. Wijeyeratne YD, et al. Anti-platelet therapy: ADP receptor antagonists. Br J Clin Pharmacol. 2011 Oct;72(4):647-57.
[2]. Sugidachi A, et al. The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel's active metabolite. J Thromb Haemost. 2007 Jul;5(7):1545-51. |
Molecular Formula |
C20H20FNO3S
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Molecular Weight |
373.44
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CAS # |
150322-43-3
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Related CAS # |
389574-19-0; 389574-20-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(OC(S1)=CC2=C1CCN(C(C3=CC=CC=C3F)C(C4CC4)=O)C2)=O
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InChi Key |
DTGLZDAWLRGWQN-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H20FNO3S/c1-12(23)25-18-10-14-11-22(9-8-17(14)26-18)19(20(24)13-6-7-13)15-4-2-3-5-16(15)21/h2-5,10,13,19H,6-9,11H2,1H3
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Chemical Name |
5-(2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate
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Synonyms |
CS-747; LY-640315; PCR-4099; CS747; LY640315; PCR4099; CS 747; LY 640315; PCR 4099; trade name Effient; Prasita
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.69 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 25.0 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: ≥ 2.5 mg/mL (6.69 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 25.0 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: ≥ 2.5 mg/mL (6.69 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 | 2.6778 mL | 13.3890 mL | 26.7781 mL | |
5 mM | 0.5356 mL | 2.6778 mL | 5.3556 mL | |
10 mM | 0.2678 mL | 1.3389 mL | 2.6778 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.