| Size | Price | Stock | Qty |
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| Targets |
P2Y12 Receptor
As a labeled version of Prasugrel, this compound targets the P2Y12 receptor on platelets. Prasugrel (non-labeled) is a potent, orally active, thienopyridine prodrug that irreversibly inhibits the P2Y12 receptor. The active metabolite of Prasugrel forms a disulfide bridge with the P2Y12 receptor, blocking ADP-induced platelet aggregation. Prasugrel-d3 is presumed to have identical pharmacological activity to the parent compound. |
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Prasugrel-d3 is not used in activity studies but serves as an analytical standard. The biological activity of its non-labeled parent, Prasugrel, is well-characterized. Prasugrel is a potent P2Y12 receptor antagonist that inhibits ADP-induced platelet aggregation with an IC50 in the low nanomolar range for its active metabolite. Prasugrel-d3 is chemically identical in terms of receptor binding, but its utility is in detection rather than pharmacology. |
| ln Vivo |
The in vivo activity of Prasugrel-d3 is assumed to be identical to that of Prasugrel, as the deuterium label is stable and has a negligible kinetic isotope effect. However, this labeled compound is not intended for in vivo efficacy studies. It is used as an internal standard to accurately measure the concentration of the parent drug in pharmacokinetic studies, ensuring precise and reproducible quantification.
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| Enzyme Assay |
Prasugrel-d3 serves as an internal standard in bioanalytical methods. The protocol for its use in a competitive binding assay would involve a radioligand binding assay. Platelet membranes expressing the P2Y12 receptor are incubated with a radiolabeled antagonist (e.g., [3H]-2-methylthio-ADP) and a fixed, known concentration of Prasugrel-d3. The unlabeled Prasugrel (analyte) and the fixed concentration of deuterated Prasugrel compete for the same binding site. Quantitation is performed by LC-MS/MS, not by the binding signal itself.
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| Cell Assay |
There are no specific cell-based protocols for Prasugrel-d3 as a test article. The cellular activity of the parent compound is assessed via platelet aggregation assays. Human platelet-rich plasma (PRP) is incubated with the active metabolite of Prasugrel. Prasugrel-d3 would be spiked into the PRP at a known concentration to serve as a quality control standard to monitor the conversion of the prodrug to its active metabolite. Cells are not typically used with this compound, as its primary role is analytical.
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| Animal Protocol |
Prasugrel-d3 is not used for in vivo efficacy studies due to its role as an internal standard. An in vivo protocol for the unlabeled parent involves the ferric chloride-induced arterial thrombosis model in rats. Male Sprague-Dawley rats are given an oral loading dose of Prasugrel (40 mg/kg) followed by 5 mg/kg/day. Carotid artery thrombosis is induced, and blood flow is monitored. This labeled compound would be used to analyze the plasma concentrations of the unlabeled parent in such a study.
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| ADME/Pharmacokinetics |
As an internal standard, Prasugrel-d3 is not studied for its own pharmacokinetics. The unlabeled parent, Prasugrel, is a prodrug. It is rapidly absorbed and metabolized by carboxylesterase 2 (CES2) in the intestine and liver to its active metabolite, R-138727. The active metabolite has a T1/2 of about 3-6 hours. It is primarily excreted in urine. Prasugrel-d3, being chemically identical, would mimic these ADME properties, making it an ideal internal standard.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Prasugrel-d3 is not applicable, as it is used in minute, non-toxic quantities in analytical applications. The parent drug, Prasugrel (brand name Effient), has a well-established clinical safety profile. Its most significant adverse effect is bleeding, which can be severe. Other common side effects include dyspnea (shortness of breath), hypotension, and gastrointestinal issues. It is contraindicated in patients with a history of stroke or transient ischemic attack (TIA).
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| References | |
| Additional Infomation |
Prasugrel-d3 is a research-grade chemical and is not approved for clinical use. It is exclusively used as an internal standard for the quantification of Prasugrel in regulated bioanalysis. Its structure is acetic-2,2,2-d3 acid, 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl ester. Its CAS number is 1127253-02-4. The use of a deuterated internal standard corrects for variations in sample preparation, recovery, and matrix effects.
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| Molecular Formula |
C20H17D3FNO3S
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|---|---|
| Molecular Weight |
376.46
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| Exact Mass |
376.134
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| CAS # |
1127253-02-4
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| Related CAS # |
Prasugrel;150322-43-3
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| PubChem CID |
25222473
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| Appearance |
White to off-white solid powder
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| LogP |
3.828
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
555
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])C(=O)OC1=CC2=C(S1)CCN(C2)C(C3=CC=CC=C3F)C(=O)C4CC4
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| InChi Key |
DTGLZDAWLRGWQN-FIBGUPNXSA-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/i1D3
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| Chemical Name |
[5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-2-yl] 2,2,2-trideuterioacetate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6563 mL | 13.2816 mL | 26.5632 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3126 mL | |
| 10 mM | 0.2656 mL | 1.3282 mL | 2.6563 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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