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Purity: ≥98%
Prasugrel Hydrochloride (formerly also known as CS-747, PCR 4099 and LY640315), a piperazine derivative, is a novel and potent thienopyridine ADP receptor (P2Y12) antagonist used for the reduction of thrombotic cardiovascular events. Prasugrel was also approved for use in Europe in February 2009. On July 10, 2009, the FDA approved the use of prasugrel for the reduction of thrombotic cardiovascular events in patients with acute coronary syndrome who are to be managed with PCI.
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| ln Vivo |
With an IC50 value of 1.8 μM, the active metabolite of prasugrel hydrochloride inhibits the in vitro platelet aggregation generated by adenosine ADP (10μM) in rat platelets[2]. In vivo, prasugrel hydrochloride exhibits a greater potency and works more quickly than clopidogrel. The active antiplatelet metabolite of prasugrel hydrochloride is produced by metabolic breakdown of the inactive prodrug in vivo. From the stomach, prasugrel hydrochloride is quickly absorbed. Maximum plasma levels of the active metabolite are reached within 1 hour following oral administration of standard-loading dosages of 60 mg, and maximal inhibition of platelet aggregation occurs within 1-2 hours[1].
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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 |
C20H21CLFNO3S
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|---|---|
| Molecular Weight |
409.9004
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| Exact Mass |
409.0915
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| CAS # |
389574-19-0
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| Related CAS # |
Prasugrel;150322-43-3;Prasugrel (Maleic acid);389574-20-3;Prasugrel-d5;1127252-92-9
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| SMILES |
FC1=CC=CC=C1C(N2CCC3=C(C=C(OC(C)=O)S3)C2)C(C4CC4)=O.[H]Cl
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| Chemical Name |
Ethanone, 2-(2-(acetyloxy)-6,7-dihydrothieno(3,2-c)pyridin-5(4H)-yl)-1-cyclopropyl-2-(2-fluorophenyl)-, hydrochloride
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| Synonyms |
Prasugrel HydrochloridePrasugrel HClCS-747CS747CS 747PCR-4099PCR4099PCR 4099LY-640315LY640315LY 640315
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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 : ~41.67 mg/mL (~101.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.07 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 20.8 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: ≥ 2.08 mg/mL (5.07 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 20.8 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: ≥ 2.08 mg/mL (5.07 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 | 2.4396 mL | 12.1981 mL | 24.3962 mL | |
| 5 mM | 0.4879 mL | 2.4396 mL | 4.8792 mL | |
| 10 mM | 0.2440 mL | 1.2198 mL | 2.4396 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.
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